<?xml version="1.0" encoding="UTF-8"?><xml><records><record><source-app name="Biblio" version="7.x">Drupal-Biblio</source-app><ref-type>17</ref-type><contributors><authors><author><style face="normal" font="default" size="100%">Shaikh, Mubarak H.</style></author><author><style face="normal" font="default" size="100%">Subhedar, Dnyaneshwar D.</style></author><author><style face="normal" font="default" size="100%">Nawale, Laxman</style></author><author><style face="normal" font="default" size="100%">Sarkar, Dhiman</style></author><author><style face="normal" font="default" size="100%">Khan, Firoz A. Kalam</style></author><author><style face="normal" font="default" size="100%">Sangshetti, Jaiprakash N.</style></author><author><style face="normal" font="default" size="100%">Shingate, Bapurao B.</style></author></authors></contributors><titles><title><style face="normal" font="default" size="100%">1,2,3-Triazole derivatives as antitubercular agents: synthesis, biological evaluation and molecular docking study</style></title><secondary-title><style face="normal" font="default" size="100%">MedChemComm</style></secondary-title></titles><dates><year><style  face="normal" font="default" size="100%">2015</style></year><pub-dates><date><style  face="normal" font="default" size="100%">MAY</style></date></pub-dates></dates><number><style face="normal" font="default" size="100%">6</style></number><publisher><style face="normal" font="default" size="100%">ROYAL SOC CHEMISTRY</style></publisher><pub-location><style face="normal" font="default" size="100%">THOMAS GRAHAM HOUSE, SCIENCE PARK, MILTON RD, CAMBRIDGE CB4 0WF, CAMBS, ENGLAND</style></pub-location><volume><style face="normal" font="default" size="100%">6</style></volume><pages><style face="normal" font="default" size="100%">1104-1116</style></pages><language><style face="normal" font="default" size="100%">eng</style></language><abstract><style face="normal" font="default" size="100%">&lt;p&gt;Searching for new active molecules against Mycobacterium tuberculosis (MTB) H37Ra, a small focused library of 1,2,3-triazoles has been efficiently prepared via a click chemistry approach. The newly synthesized compounds were tested against drug-sensitive MTB. Several derivatives were found to be promising inhibitors of MTB characterized by lower MIC values (5.8-29.9 mu g mL(-1)). Among all the synthesized 31 compounds, 15e was the most active compound against MTB. Based on the results from the antitubercular activity, SAR for the synthesized series has been developed. The active compounds from the anti-tubercular study were further tested for anti-proliferative activity against THP-1, A549 and PANC-1 cell lines using MTT assay and showed no significant cytotoxic activity against these three cell lines except THP-1 at the maximum concentration evaluated. Further, the synthesized compounds were found to have potential antioxidant activities with an IC50 range of 10.1-37.3 mu g mL(-1). The molecular docking study of the synthesized compounds was performed against the DprE1 enzyme of MTB to understand the binding interactions. Moreover, the synthesized compounds were also analysed for ADME properties and all the experimental results promote us to consider this series as a starting point for the development of novel and more potent anti-tubercular agents in the future.&lt;/p&gt;</style></abstract><issue><style face="normal" font="default" size="100%">6</style></issue><work-type><style face="normal" font="default" size="100%">Article</style></work-type><custom3><style face="normal" font="default" size="100%">&lt;p&gt;Foreign&lt;/p&gt;</style></custom3><custom4><style face="normal" font="default" size="100%">&lt;p&gt;2.319&lt;/p&gt;</style></custom4></record><record><source-app name="Biblio" version="7.x">Drupal-Biblio</source-app><ref-type>47</ref-type><contributors><authors><author><style face="normal" font="default" size="100%">Nawale, Laxman</style></author><author><style face="normal" font="default" size="100%">Sarkar, Dhiman</style></author></authors></contributors><titles><title><style face="normal" font="default" size="100%">Discovery of new chemical entities against diseases of national importance :an HTS approach</style></title><secondary-title><style face="normal" font="default" size="100%">National Science Day, At CSIR-NCL</style></secondary-title></titles><dates><year><style  face="normal" font="default" size="100%">2015</style></year><pub-dates><date><style  face="normal" font="default" size="100%">FEB</style></date></pub-dates></dates><pub-location><style face="normal" font="default" size="100%">Combi Chem-Bio Resource Center, OCD, National Chemical Laboratory, Pune - 411 008</style></pub-location><language><style face="normal" font="default" size="100%">eng</style></language></record><record><source-app name="Biblio" version="7.x">Drupal-Biblio</source-app><ref-type>47</ref-type><contributors><authors><author><style face="normal" font="default" size="100%">Nawale, Laxman</style></author><author><style face="normal" font="default" size="100%">Sarkar, Dhiman</style></author></authors></contributors><titles><title><style face="normal" font="default" size="100%">Efficacy study of potential anti-tubercular molecules: in-vitro and ex-vivo</style></title><secondary-title><style face="normal" font="default" size="100%">National Science Day</style></secondary-title></titles><dates><year><style  face="normal" font="default" size="100%">2015</style></year><pub-dates><date><style  face="normal" font="default" size="100%">FEB</style></date></pub-dates></dates><pub-location><style face="normal" font="default" size="100%">National Chemical Laboratory, Pune 411008</style></pub-location><language><style face="normal" font="default" size="100%">eng</style></language><abstract><style face="normal" font="default" size="100%">&lt;p&gt;Tuberculosis: Infectious disease caused by the bacillus Mycobacterium tuberculosis Second leading infectious killer after HIV/AIDS In 2013, 8.6 million TB cases were reported out of which 1.3 million died Emergence of Multi-drug resistant TB (MDR-TB) and extremely drug resistant TB (XDR) for which no drugs are available. Latency being a cause of recurring TB infection is a major problem in eradication of TB&lt;/p&gt;</style></abstract></record><record><source-app name="Biblio" version="7.x">Drupal-Biblio</source-app><ref-type>47</ref-type><contributors><authors><author><style face="normal" font="default" size="100%">Manek, Hardik</style></author><author><style face="normal" font="default" size="100%">Nawale, Laxman</style></author><author><style face="normal" font="default" size="100%">Jadhav, Nandadeep J.</style></author><author><style face="normal" font="default" size="100%">Sarkar, Dhiman</style></author></authors></contributors><titles><title><style face="normal" font="default" size="100%">High throughput screening of inhibitors for tuberculosis at NCL : a novel drug discovery initiative from CSIR</style></title><secondary-title><style face="normal" font="default" size="100%">73rd CSIR Foundation Day, at CSIR-National Chemical Laboratory, Pune</style></secondary-title></titles><dates><year><style  face="normal" font="default" size="100%">2015</style></year><pub-dates><date><style  face="normal" font="default" size="100%">SEP</style></date></pub-dates></dates><publisher><style face="normal" font="default" size="100%">CSIR-National Chemical Laboratory, Pune</style></publisher><pub-location><style face="normal" font="default" size="100%">CSIR-National Chemical Laboratory, Pune</style></pub-location><language><style face="normal" font="default" size="100%">eng</style></language><abstract><style face="normal" font="default" size="100%">&lt;p&gt;Discover and develop novel drugs that are effective at curing latent, drug sensitive and drug resistant TB Study the biology of tuberculosis bacilli in great detail to identify new metabolic pathways that may be vulnerable to drugs Test thousands of potential drugs in our screening facility to find new compounds or new compound classes that kill TB bacteria Increase throughput up to 20,000 compounds at a time Develop novel screens using conditions that mimic those the TB bacteria encounters in the human body Utilize medical chemistry to optimize the structures of compounds so that they kill TB bacteria in a more potent fashion and are non-toxic Meet the challenges from industry&lt;/p&gt;</style></abstract></record><record><source-app name="Biblio" version="7.x">Drupal-Biblio</source-app><ref-type>47</ref-type><contributors><authors><author><style face="normal" font="default" size="100%">Dubey, Parul</style></author><author><style face="normal" font="default" size="100%">Nawale, Laxman</style></author><author><style face="normal" font="default" size="100%">Sarkar, Dhiman</style></author><author><style face="normal" font="default" size="100%">Nisal, Anuya</style></author><author><style face="normal" font="default" size="100%">Prabhune, Asmita</style></author></authors></contributors><titles><title><style face="normal" font="default" size="100%">Mechanistic understanding of rapid gelation of silk fibroin using a biosurfactant – sophorolipid</style></title><secondary-title><style face="normal" font="default" size="100%">National Science Day, At CSIR-NCL</style></secondary-title></titles><dates><year><style  face="normal" font="default" size="100%">2015</style></year><pub-dates><date><style  face="normal" font="default" size="100%">FEB</style></date></pub-dates></dates><pub-location><style face="normal" font="default" size="100%">National Chemical Laboratory, Pune  India</style></pub-location><language><style face="normal" font="default" size="100%">eng</style></language><abstract><style face="normal" font="default" size="100%">&lt;p&gt;3D polymeric hydrogels find use in biomedical applications as scaffolds and drug delivery vehicle • Silk fibroin a structural protein is a promising candidate (excellent thermo-mechanicals, biocompatibility, biodegradability) • Sophorolipid (SL)-a biosurfactant is known to exhibit antimicrobial, anti cancerous and cell differentiating. • Use of SL as gelling agent can enhance the applicability of SF hydrogels • SF-SL scaffolds obtained by lyophilization of hydrogels can find application in tissue regeneration&lt;/p&gt;</style></abstract></record><record><source-app name="Biblio" version="7.x">Drupal-Biblio</source-app><ref-type>17</ref-type><contributors><authors><author><style face="normal" font="default" size="100%">Said, Madhukar S.</style></author><author><style face="normal" font="default" size="100%">Chinchansure, Ashish A.</style></author><author><style face="normal" font="default" size="100%">Nawale, Laxman</style></author><author><style face="normal" font="default" size="100%">Durge, Ankita</style></author><author><style face="normal" font="default" size="100%">Wadhwani, Ashish</style></author><author><style face="normal" font="default" size="100%">Kulkarni, Smita S.</style></author><author><style face="normal" font="default" size="100%">Sarkar, Dhiman</style></author><author><style face="normal" font="default" size="100%">Joshi, Swati P.</style></author></authors></contributors><titles><title><style face="normal" font="default" size="100%">New butenolide cinnamate and other biological active chemical constituents from Polygonum glabrum</style></title><secondary-title><style face="normal" font="default" size="100%">Natural Product Research</style></secondary-title></titles><keywords><keyword><style  face="normal" font="default" size="100%">anti-HIV-1</style></keyword><keyword><style  face="normal" font="default" size="100%">anti-mycobacterium</style></keyword><keyword><style  face="normal" font="default" size="100%">antiproliferative</style></keyword><keyword><style  face="normal" font="default" size="100%">phytochemicals</style></keyword><keyword><style  face="normal" font="default" size="100%">Polygonaceae</style></keyword><keyword><style  face="normal" font="default" size="100%">Polygonum glabrum</style></keyword></keywords><dates><year><style  face="normal" font="default" size="100%">2015</style></year><pub-dates><date><style  face="normal" font="default" size="100%">NOV</style></date></pub-dates></dates><number><style face="normal" font="default" size="100%">22</style></number><publisher><style face="normal" font="default" size="100%">TAYLOR &amp; FRANCIS LTD</style></publisher><pub-location><style face="normal" font="default" size="100%">4 PARK SQUARE, MILTON PARK, ABINGDON OX14 4RN, OXON, ENGLAND</style></pub-location><volume><style face="normal" font="default" size="100%">29</style></volume><pages><style face="normal" font="default" size="100%">2080-2086</style></pages><language><style face="normal" font="default" size="100%">eng</style></language><abstract><style face="normal" font="default" size="100%">&lt;p&gt;Phytochemical investigation of the methanol extract of the aerial parts of Polygonum glabrum afforded one new natural product (-)-2-methoxy-2-butenolide-3-cinnamate (1) along with six known compounds, -hydroxyfriedalanol (2), 3-hydroxy-5-methoxystilbene (3), (-) pinocembrin (4), sitosterol-(6-O-palmitoyl)-3-O–d-glucopyranoside (5), (-) pinocembrin-5-methyl ether (6) and sitosterol-3-O–d-glucopyranoside (7). Compound 1 showed promising in vitro anti-HIV-1 activity against primary isolates HIV-1(UG070) (X4, subtype D) and HIV-1(VB59) (R5, subtype C) assayed using TZM-bl cell line with IC50 in the range of 15.68-22.43g/mL. The extract showed TI in the range of 19.19-27.37 with IC50 in the range of 10.90-15.55g/mL. Compounds 1, 3 and 4 exhibited in vitro anti-mycobacterium activity against Mycobacterium tuberculosis H37Ra with IC50 values of 1.43, 3.33 and 1.11g/mL in dormant phase and 2.27, 3.33 and 1.21g/mL in active phase, respectively. Compound 4 was found to be the most active antiproliferative with IC50 values of 1.88-11.00g/mL against THP-1, A549, Panc-1, HeLa and MCF7 cell lines.&lt;/p&gt;</style></abstract><issue><style face="normal" font="default" size="100%">22</style></issue><custom3><style face="normal" font="default" size="100%">&lt;p&gt;Foreign&lt;/p&gt;</style></custom3><custom4><style face="normal" font="default" size="100%">1.057</style></custom4></record><record><source-app name="Biblio" version="7.x">Drupal-Biblio</source-app><ref-type>47</ref-type><contributors><authors><author><style face="normal" font="default" size="100%">Singh, Ruby</style></author><author><style face="normal" font="default" size="100%">Nawale, Laxman</style></author><author><style face="normal" font="default" size="100%">Gaikwad, Sushama M.</style></author><author><style face="normal" font="default" size="100%">Suresha, C. G.</style></author></authors></contributors><titles><title><style face="normal" font="default" size="100%">Purification and characterization of an agglutinin from datura innoxia with antineoplastic activity</style></title><secondary-title><style face="normal" font="default" size="100%">National Science Day, At CSIR-NCL</style></secondary-title></titles><dates><year><style  face="normal" font="default" size="100%">2015</style></year><pub-dates><date><style  face="normal" font="default" size="100%">FEB</style></date></pub-dates></dates><pub-location><style face="normal" font="default" size="100%">CSIR-National Chemical Laboratory, Pune 411008, India</style></pub-location><language><style face="normal" font="default" size="100%">eng</style></language><abstract><style face="normal" font="default" size="100%">&lt;p&gt;Lectins are carbohydrate binding proteins of non-immune origin. Due to their multivalency, lectins can be easily detected using agglutination. Lectins are reported to induce cytotoxicity or inhibition of growth in various cancer cells., hence good therapeutic startegy against cancer. Factors such as specificity, stability, assay rapidity, and costs combine to make lectins attractive diagnostic reagents. Datura innoxia belongs to family of Solanaceae.All parts of the plant are hallucinogenic, hypnotic and narcotic. Application: at low dose acts as pain killer, relieves asthma and rheumatism.&lt;/p&gt;</style></abstract></record><record><source-app name="Biblio" version="7.x">Drupal-Biblio</source-app><ref-type>47</ref-type><contributors><authors><author><style face="normal" font="default" size="100%">Nawale, Laxman</style></author><author><style face="normal" font="default" size="100%">Sarkar, Dhiman</style></author></authors></contributors><titles><title><style face="normal" font="default" size="100%">Quantitative, automated, high content screening assay approach to anti-angiogenicdrug discovery</style></title><secondary-title><style face="normal" font="default" size="100%">National Science Day, At CSIR-NCL</style></secondary-title></titles><dates><year><style  face="normal" font="default" size="100%">2015</style></year><pub-dates><date><style  face="normal" font="default" size="100%">FEB</style></date></pub-dates></dates><pub-location><style face="normal" font="default" size="100%">Combi Chem-Bio Resource Center, OCD, National Chemical Laboratory, Pune - 411 008</style></pub-location><language><style face="normal" font="default" size="100%">eng</style></language><abstract><style face="normal" font="default" size="100%">&lt;p&gt;Angiogenesisenhancescancer,maculardegeneration,etc.. Currentangiogenicassays--indirect,manual,timeconsuming,laborintensive,difficulttoquantify,andexpensive. Wedevelopedanautomated,quantitative,HighContentScreeningangiogenictubeformationassaywouldbenefitdrugdiscoveryforseveraltherapeuticareas. Humanendothelialcellswereseededwithpro-oranti-angiogeniccompoundsonaMatrigelTMlayerina96-wellplate.Afterangiogenictubesformation,thepositivecontrolsandthetestsampleswerefixed,fluorescentlylabeled,automaticallyimagedonCellomics’ArrayScan®HCSReader,andquantitativelyanalyzedon-the-flybytheTubeFormationBioApplicationsoftwaremodule. Multiplefeaturesrelevantforangiogenesisandangiogenictubeformationwereautomaticallymeasured. Thisrobustandreliableassaythusenabledthelarge-scale,quantitative,screeningandcharacterizationofcompoundsaffectingbothpro-andanti-angiogenicpathways.&lt;/p&gt;</style></abstract></record><record><source-app name="Biblio" version="7.x">Drupal-Biblio</source-app><ref-type>17</ref-type><contributors><authors><author><style face="normal" font="default" size="100%">Dubey, Parul</style></author><author><style face="normal" font="default" size="100%">Nawale, Laxman</style></author><author><style face="normal" font="default" size="100%">Sarkar, Dhiman</style></author><author><style face="normal" font="default" size="100%">Nisal, Anuya</style></author><author><style face="normal" font="default" size="100%">Prabhune, Asmita</style></author></authors></contributors><titles><title><style face="normal" font="default" size="100%">Sophorolipid assisted tunable and rapid gelation of silk fibroin to form porous biomedical scaffolds</style></title><secondary-title><style face="normal" font="default" size="100%">RSC Advances</style></secondary-title></titles><dates><year><style  face="normal" font="default" size="100%">2015</style></year><pub-dates><date><style  face="normal" font="default" size="100%">MAR</style></date></pub-dates></dates><number><style face="normal" font="default" size="100%">43</style></number><publisher><style face="normal" font="default" size="100%">ROYAL SOC CHEMISTRY</style></publisher><pub-location><style face="normal" font="default" size="100%">THOMAS GRAHAM HOUSE, SCIENCE PARK, MILTON RD, CAMBRIDGE CB4 0WF, CAMBS, ENGLAND</style></pub-location><volume><style face="normal" font="default" size="100%">5</style></volume><pages><style face="normal" font="default" size="100%">33955-33962</style></pages><language><style face="normal" font="default" size="100%">eng</style></language><abstract><style face="normal" font="default" size="100%">&lt;p&gt;Three dimensional polymer hydrogels, based on both natural and synthetic polymers, are increasingly being used as scaffolds and drug delivery vehicles for biomedical applications. Fibrous protein, silk fibroin (SF), obtained from the Bombyx mori silkworm is a promising candidate in this area. However, SF has a long gelation time of about a few weeks that can only be reduced by non-physiological treatments (e. g. high temperature, ultrasonication and low pH) or by addition of a chemical and non-biodegradable polymer and/or surfactant. We report here accelerated gelation of SF under physiological conditions using a biosurfactant, sophorolipid (SL) as a gelling agent. SL and SF are completely miscible and form a very clear solution upon mixing. Hence it is interesting to see that this clear solution gels in a time span of just a few hours. The hydrogels so formed have pore architecture, porosities and mechanical stability ideally suited for tissue culture applications. Here we also demonstrate that mouse fibroblast cells not only adhere to but also extensively proliferate on these SF-SL scaffolds.&lt;/p&gt;</style></abstract><issue><style face="normal" font="default" size="100%">43</style></issue><custom3><style face="normal" font="default" size="100%">&lt;p&gt;Foreign&lt;/p&gt;</style></custom3><custom4><style face="normal" font="default" size="100%">3.289</style></custom4></record><record><source-app name="Biblio" version="7.x">Drupal-Biblio</source-app><ref-type>17</ref-type><contributors><authors><author><style face="normal" font="default" size="100%">Subhedar, Dnyaneshwar D.</style></author><author><style face="normal" font="default" size="100%">Shaikh, Mubarak H.</style></author><author><style face="normal" font="default" size="100%">Nawale, Laxman</style></author><author><style face="normal" font="default" size="100%">Yeware, Amar</style></author><author><style face="normal" font="default" size="100%">Sarkar, Dhiman</style></author><author><style face="normal" font="default" size="100%">Shingate, Bapurao B.</style></author></authors></contributors><titles><title><style face="normal" font="default" size="100%">[Et3NH][HSO4] catalyzed efficient synthesis of 5-arylidene-rhodanine conjugates and their antitubercular activity</style></title><secondary-title><style face="normal" font="default" size="100%">Research on Chemical Intermediates</style></secondary-title></titles><dates><year><style  face="normal" font="default" size="100%">2016</style></year><pub-dates><date><style  face="normal" font="default" size="100%">AUG</style></date></pub-dates></dates><volume><style face="normal" font="default" size="100%">42</style></volume><pages><style face="normal" font="default" size="100%">6607-6626</style></pages><language><style face="normal" font="default" size="100%">eng</style></language><abstract><style face="normal" font="default" size="100%">&lt;p&gt;We have described a highly efficient, safer protocol for the synthesis of 5-arylidene-rhodanine conjugates catalyzed by Bronsted acidic ionic liquid [Et3NH][HSO4] in excellent yields. The protocol offers cost-effective, environmentally benign, solvent-free conditions and recycle-reuse of the catalyst. The synthesized 5-arylidene-rhodanine conjugates were characterized on the basis of (1) H NMR, C-13 NMR and HRMS spectral data. A series of 5-arylidene-rhodanine derivatives 3a-h, 4a-h were synthesized and evaluated for their in vitro antitubercular activity against dormant Mycobacterium tuberculosis H37Ra and M. bovis BCG strains. Moreover, compounds 3a, 3b, 3e, 3f, 3g, 3h and 4f exhibited good antitubercular activity and were also evaluated for anti-proliferative activity against MCF-7, A549 and HCT116 cell lines using modified MTT assay and found to be noncytotoxic. Compounds 3a-h and 4f were further screened for their antibacterial activity against four bacteria strains to assess their selectivity towards M. tuberculosis. Furthermore, in silico ADME prediction of all the tested compounds followed the criteria for orally active drug and, therefore, these compounds may have a good potential for eventual development as oral agents.&lt;/p&gt;</style></abstract><issue><style face="normal" font="default" size="100%">8</style></issue><custom3><style face="normal" font="default" size="100%">&lt;p&gt;Foreign&lt;/p&gt;</style></custom3><custom4><style face="normal" font="default" size="100%">1.833</style></custom4></record><record><source-app name="Biblio" version="7.x">Drupal-Biblio</source-app><ref-type>17</ref-type><contributors><authors><author><style face="normal" font="default" size="100%">Subhedar, Dnyaneshwar D.</style></author><author><style face="normal" font="default" size="100%">Shaikh, Mubarak H.</style></author><author><style face="normal" font="default" size="100%">Nawale, Laxman</style></author><author><style face="normal" font="default" size="100%">Yeware, Amar</style></author><author><style face="normal" font="default" size="100%">Sarkar, Dhiman</style></author><author><style face="normal" font="default" size="100%">Khan, Firoz A. Kalam</style></author><author><style face="normal" font="default" size="100%">Sangshetti, Jaiprakash N.</style></author><author><style face="normal" font="default" size="100%">Shingate, Bapurao B.</style></author></authors></contributors><titles><title><style face="normal" font="default" size="100%">Novel tetrazoloquinoline-rhodanine conjugates: highly efficient synthesis and biological evaluation</style></title><secondary-title><style face="normal" font="default" size="100%">Bioorganic &amp; Medicinal Chemistry Letters</style></secondary-title></titles><keywords><keyword><style  face="normal" font="default" size="100%">antifungal</style></keyword><keyword><style  face="normal" font="default" size="100%">Antitubercular</style></keyword><keyword><style  face="normal" font="default" size="100%">Cytotoxicity</style></keyword><keyword><style  face="normal" font="default" size="100%">Docking study</style></keyword><keyword><style  face="normal" font="default" size="100%">Rhodanine derivatives</style></keyword></keywords><dates><year><style  face="normal" font="default" size="100%">2016</style></year><pub-dates><date><style  face="normal" font="default" size="100%">MAY</style></date></pub-dates></dates><number><style face="normal" font="default" size="100%">9</style></number><publisher><style face="normal" font="default" size="100%">PERGAMON-ELSEVIER SCIENCE LTD</style></publisher><pub-location><style face="normal" font="default" size="100%">THE BOULEVARD, LANGFORD LANE, KIDLINGTON, OXFORD OX5 1GB, ENGLAND</style></pub-location><volume><style face="normal" font="default" size="100%">26</style></volume><pages><style face="normal" font="default" size="100%">2278-2283</style></pages><language><style face="normal" font="default" size="100%">eng</style></language><abstract><style face="normal" font="default" size="100%">&lt;p&gt;In search of new active molecules against Mycobacterium tuberculosis (MTB) H37Ra and Mycobacterium bovis BCG, a small focused library of rhodanine incorporated tetrazoloquinoline has been efficiently synthesized by using [HDBU][HSO4] acidic ionic liquid. The compound 3c found to be promising inhibitor of MTB H37Ra and M. bovis BCG characterized by lower MIC values 4.5 and 2.0 mu g/mL, respectively. The active compounds were further tested for cytotoxicity against HeLa, THP-1, A549 and PANC-1 cell lines using MTT assay and showed no significant cytotoxic activity at the maximum concentration evaluated. Again, the synthesized compounds were found to have potential antifungal activity. Furthermore, to rationalize the observed biological activity data, the molecular docking study also been carried out against a potential target Zmp1 enzyme of MTB H37Ra, which revealed a significant correlation between the binding score and biological activity for these compounds. The results of in vitro and in silico study suggest that these compounds possess ideal structural requirement for the further development of novel therapeutic agents. (C) 2016 Elsevier Ltd. All rights reserved.&lt;/p&gt;</style></abstract><issue><style face="normal" font="default" size="100%">9</style></issue><custom3><style face="normal" font="default" size="100%">&lt;p&gt;Foreign&lt;/p&gt;</style></custom3><custom4><style face="normal" font="default" size="100%">&lt;p&gt;2.486&lt;/p&gt;</style></custom4></record><record><source-app name="Biblio" version="7.x">Drupal-Biblio</source-app><ref-type>17</ref-type><contributors><authors><author><style face="normal" font="default" size="100%">Subhedar, Dnyaneshwar D.</style></author><author><style face="normal" font="default" size="100%">Shaikh, Mubarak H.</style></author><author><style face="normal" font="default" size="100%">Shingate, Bapurao B.</style></author><author><style face="normal" font="default" size="100%">Nawale, Laxman</style></author><author><style face="normal" font="default" size="100%">Sarkar, Dhiman</style></author><author><style face="normal" font="default" size="100%">Khedkar, Vijay M.</style></author></authors></contributors><titles><title><style face="normal" font="default" size="100%">Novel tetrazoloquinoline-thiazolidinone conjugates as possible antitubercular agents: synthesis and molecular docking</style></title><secondary-title><style face="normal" font="default" size="100%">Medchemcomm</style></secondary-title></titles><dates><year><style  face="normal" font="default" size="100%">2016</style></year><pub-dates><date><style  face="normal" font="default" size="100%">JUL</style></date></pub-dates></dates><volume><style face="normal" font="default" size="100%">7</style></volume><pages><style face="normal" font="default" size="100%">1832-1848</style></pages><language><style face="normal" font="default" size="100%">eng</style></language><abstract><style face="normal" font="default" size="100%">&lt;p&gt;A novel approach for the synthesis of a new 4-thiazolidinone scaffold was developed by a one-pot three-component cyclocondensation of various tetrazolo quinoline aldehydes 1a-f, acid hydrazide 2a-c, and thioglycolic acid 3 in the presence of [DBUH].OAc] as a catalyst in high yields. All the conjugates were screened for their antimycobacterial activity against MTB H37Ra and M. bovis BCG strains, with the MIC values ranging from 0.99-13.55 mu mol mL(-1) and 0.14-20.11 mu mol mL(-1), respectively. The 4-thiazolidinone-incorporated tetrazoloquinoline derivatives 4a, 4d, 4g, 4j, 4m, and 4p were highly potent against MTB H37Ra and M. bovis BCG strains. The most active compounds were also evaluated for their cytotoxicity against MCF-7, A549, and HCT 116 cell lines and were found to be non-cytotoxic. Further, molecular docking studies into the active site of the InhA enzyme revealed a similar binding mode to the native ligand in the crystal structure, thereby helping us to understand the ligand-protein binding interaction and establish a structural basis for the inhibition of mycobacterium tuberculosis. The results suggest that the tetrazoloquinoline-thiazolidinone conjugates 4a, 4d, 4g, 4j, 4m, and 4p are promising antitubercular agents.&lt;/p&gt;</style></abstract><issue><style face="normal" font="default" size="100%">9</style></issue><custom3><style face="normal" font="default" size="100%">&lt;p&gt;Foreign&lt;/p&gt;</style></custom3><custom4><style face="normal" font="default" size="100%">2.319</style></custom4></record><record><source-app name="Biblio" version="7.x">Drupal-Biblio</source-app><ref-type>17</ref-type><contributors><authors><author><style face="normal" font="default" size="100%">Singh, Richa</style></author><author><style face="normal" font="default" size="100%">Nawale, Laxman</style></author><author><style face="normal" font="default" size="100%">Arkile, Manisha A.</style></author><author><style face="normal" font="default" size="100%">Wadhwani, Sweety</style></author><author><style face="normal" font="default" size="100%">Shedbalkar, Utkarsha</style></author><author><style face="normal" font="default" size="100%">Chopade, Snehal</style></author><author><style face="normal" font="default" size="100%">Sarkar, Dhiman</style></author><author><style face="normal" font="default" size="100%">Chopade, Balu Ananda</style></author></authors></contributors><titles><title><style face="normal" font="default" size="100%">Phytogenic silver, gold, and bimetallic nanoparticles as novel antitubercular agents</style></title><secondary-title><style face="normal" font="default" size="100%">International Journal of Nanomedicine</style></secondary-title></titles><keywords><keyword><style  face="normal" font="default" size="100%">Antimycobacterial agent</style></keyword><keyword><style  face="normal" font="default" size="100%">Cytotoxicity</style></keyword><keyword><style  face="normal" font="default" size="100%">drug resistance</style></keyword><keyword><style  face="normal" font="default" size="100%">Mycobacteria</style></keyword><keyword><style  face="normal" font="default" size="100%">Nanoparticles</style></keyword><keyword><style  face="normal" font="default" size="100%">tuberculosis</style></keyword></keywords><dates><year><style  face="normal" font="default" size="100%">2016</style></year><pub-dates><date><style  face="normal" font="default" size="100%">MAY</style></date></pub-dates></dates><publisher><style face="normal" font="default" size="100%">DOVE MEDICAL PRESS LTD</style></publisher><pub-location><style face="normal" font="default" size="100%">PO BOX 300-008, ALBANY, AUCKLAND 0752, NEW ZEALAND</style></pub-location><volume><style face="normal" font="default" size="100%">11</style></volume><pages><style face="normal" font="default" size="100%">1889—1897</style></pages><language><style face="normal" font="default" size="100%">eng</style></language><abstract><style face="normal" font="default" size="100%">&lt;p&gt;Purpose: Multi- and extensively drug-resistant tuberculosis (TB) is a global threat to human health. It requires immediate action to seek new antitubercular compounds and devise alternate strategies. Nanomaterials, in the present scenario, have opened new avenues in medicine, diagnosis, and therapeutics. In view of this, the current study aims to determine the efficacy of phytogenic metal nanoparticles to inhibit mycobacteria. Methods: Silver (AgNPs), gold (AuNPs), and gold-silver bimetallic (Au-AgNPs) nanoparticles synthesized from medicinal plants, such as Barleria prionitis, Plumbago zeylanica, and Syzygium cumini, were tested against Mycobacterium tuberculosis and M. bovis BCG. In vitro and ex vivo macrophage infection model assays were designed to determine minimum inhibitory concentration (MIC) and half maximal inhibitory concentration of nanoparticles. Microscopic analyses were carried out to demonstrate intracellular uptake of nanoparticles in macrophages. Besides this, biocompatibility, specificity, and selectivity of nanoparticles were also established with respect to human cell lines. Results: Au-AgNPs exhibited highest antitubercular activity, with MIC of &amp;lt;2.56 mu g/mL, followed by AgNPs. AuNPs did not show such activity at concentrations of up to 100 mu g/mL. In vitro and ex vivo macrophage infection model assays revealed the inhibition of both active and dormant stage mycobacteria on exposure to Au-AgNPs. These nanoparticles were capable of entering macrophage cells and exhibited up to 45% cytotoxicity at 30 mu g/mL (ten times MIC concentration) after 48 hours. Among these, Au-AgNPs synthesized from S. cumini were found to be more specific toward mycobacteria, with their selectivity index in the range of 94-108. Conclusion: This is the first study to report the antimycobacterial activity of AuNPs, AgNPs, and Au-AgNPs synthesized from medicinal plants. Among these, Au-AgNPs from S. cumini showed profound efficiency, specificity, and selectivity to kill mycobacteria. These should be investigated further to develop novel TB nanoantibiotics.&lt;/p&gt;</style></abstract><custom3><style face="normal" font="default" size="100%">&lt;p&gt;Foreign&lt;/p&gt;</style></custom3><custom4><style face="normal" font="default" size="100%">4.32</style></custom4></record><record><source-app name="Biblio" version="7.x">Drupal-Biblio</source-app><ref-type>17</ref-type><contributors><authors><author><style face="normal" font="default" size="100%">Shaikh, Mubarak H.</style></author><author><style face="normal" font="default" size="100%">Subhedar, Dnyaneshwar D.</style></author><author><style face="normal" font="default" size="100%">Shingate, Bapurao B.</style></author><author><style face="normal" font="default" size="100%">Khan, Firoz A. Kalam</style></author><author><style face="normal" font="default" size="100%">Sangshetti, Jaiprakash N.</style></author><author><style face="normal" font="default" size="100%">Khedkar, Vijay M.</style></author><author><style face="normal" font="default" size="100%">Nawale, Laxman</style></author><author><style face="normal" font="default" size="100%">Sarkar, Dhiman</style></author><author><style face="normal" font="default" size="100%">Navale, Govinda R.</style></author><author><style face="normal" font="default" size="100%">Shinde, Sandip S.</style></author></authors></contributors><titles><title><style face="normal" font="default" size="100%">Synthesis, biological evaluation and molecular docking of novel coumarin incorporated triazoles as antitubercular, antioxidant and antimicrobial agents</style></title><secondary-title><style face="normal" font="default" size="100%">Medicinal Chemistry Research</style></secondary-title></titles><keywords><keyword><style  face="normal" font="default" size="100%">1</style></keyword><keyword><style  face="normal" font="default" size="100%">2</style></keyword><keyword><style  face="normal" font="default" size="100%">3-Triazole</style></keyword><keyword><style  face="normal" font="default" size="100%">ADME prediction</style></keyword><keyword><style  face="normal" font="default" size="100%">Antimicrobial</style></keyword><keyword><style  face="normal" font="default" size="100%">Antioxidant</style></keyword><keyword><style  face="normal" font="default" size="100%">Antitubercular</style></keyword><keyword><style  face="normal" font="default" size="100%">Click chemistry</style></keyword><keyword><style  face="normal" font="default" size="100%">Docking study</style></keyword></keywords><dates><year><style  face="normal" font="default" size="100%">2016</style></year><pub-dates><date><style  face="normal" font="default" size="100%">APR</style></date></pub-dates></dates><number><style face="normal" font="default" size="100%">4</style></number><publisher><style face="normal" font="default" size="100%">SPRINGER BIRKHAUSER</style></publisher><pub-location><style face="normal" font="default" size="100%">233 SPRING STREET, 6TH FLOOR, NEW YORK, NY 10013 USA</style></pub-location><volume><style face="normal" font="default" size="100%">25</style></volume><pages><style face="normal" font="default" size="100%">790-804</style></pages><language><style face="normal" font="default" size="100%">eng</style></language><abstract><style face="normal" font="default" size="100%">&lt;p&gt;A series of new coumarin-based 1,2,3-triazole derivatives were designed, synthesized and evaluated for their antitubercular activity in vitro against Mycobacterium tuberculosis H37Ra, antioxidant activity by DPPH radical scavenging assay, antimicrobial activity in vitro against three gram-positive bacteria (Staphylococcus aureus, Micrococcus luteus and Bacillus cereus) and three gram-negative bacteria (Escherichia coli, Pseudomonas fluorescens and Flavobacterium devorans as well as three fungi (Aspergillus niger, Penicillium chrysogenum and Curvularia lunata). The bioactive assay showed that some synthesized coumarin triazoles displayed comparable or even better antitubercular, antioxidant, antibacterial and antifungal efficacy in comparison with reference drugs. Furthermore, docking study has been performed against DprE1 enzyme of M. tuberculosis that showed good binding interactions. Moreover, the synthesized compounds were also analyzed for ADME properties and showed potential to build up as good oral drug candidates. New coumarin-based 1,2,3-triazole derivatives were designed, synthesized and evaluated for their antitubercular, antioxidant, antibacterial and antifungal activity. Some of the coumarin-based triazole derivatives displayed comparable or even better efficacy in comparison with reference drugs. Molecular docking study has been performed against DprE1 enzyme of Mycobacterium tuberculosis showed good binding interactions. [GRAPHICS] .&lt;/p&gt;</style></abstract><issue><style face="normal" font="default" size="100%">4</style></issue><custom3><style face="normal" font="default" size="100%">&lt;p&gt;Foreign&lt;/p&gt;</style></custom3><custom4><style face="normal" font="default" size="100%">1.436</style></custom4></record><record><source-app name="Biblio" version="7.x">Drupal-Biblio</source-app><ref-type>17</ref-type><contributors><authors><author><style face="normal" font="default" size="100%">Desai, N. C.</style></author><author><style face="normal" font="default" size="100%">Somani, Hardik</style></author><author><style face="normal" font="default" size="100%">Trivedi, Amit</style></author><author><style face="normal" font="default" size="100%">Bhatt, Kandarp</style></author><author><style face="normal" font="default" size="100%">Nawale, Laxman</style></author><author><style face="normal" font="default" size="100%">Khedkar, Vijay M.</style></author><author><style face="normal" font="default" size="100%">Jha, Prakash C.</style></author><author><style face="normal" font="default" size="100%">Sarkar, Dhiman</style></author></authors></contributors><titles><title><style face="normal" font="default" size="100%">Synthesis, biological evaluation and molecular docking study of some novel indole and pyridine based 1,3,4-oxadiazole derivatives as potential antitubercular agents</style></title><secondary-title><style face="normal" font="default" size="100%">Bioorganic &amp; Medicinal Chemistry Letters</style></secondary-title></titles><keywords><keyword><style  face="normal" font="default" size="100%">1</style></keyword><keyword><style  face="normal" font="default" size="100%">3</style></keyword><keyword><style  face="normal" font="default" size="100%">4-Oxadiazole</style></keyword><keyword><style  face="normal" font="default" size="100%">Antitubercular activity</style></keyword><keyword><style  face="normal" font="default" size="100%">Cytotoxicity</style></keyword><keyword><style  face="normal" font="default" size="100%">Indole</style></keyword><keyword><style  face="normal" font="default" size="100%">Molecular docking</style></keyword><keyword><style  face="normal" font="default" size="100%">Pyridine</style></keyword></keywords><dates><year><style  face="normal" font="default" size="100%">2016</style></year><pub-dates><date><style  face="normal" font="default" size="100%">APR </style></date></pub-dates></dates><number><style face="normal" font="default" size="100%">7</style></number><publisher><style face="normal" font="default" size="100%">PERGAMON-ELSEVIER SCIENCE LTD</style></publisher><pub-location><style face="normal" font="default" size="100%">THE BOULEVARD, LANGFORD LANE, KIDLINGTON, OXFORD OX5 1GB, ENGLAND</style></pub-location><volume><style face="normal" font="default" size="100%">26</style></volume><pages><style face="normal" font="default" size="100%">1776-1783</style></pages><language><style face="normal" font="default" size="100%">eng</style></language><abstract><style face="normal" font="default" size="100%">&lt;p&gt;A series of indole and pyridine based 1,3,4-oxadiazole derivatives 5a-t were synthesized and evaluated for their in vitro antitubercular activity against Mycobacterium tuberculosis H37Ra (MTB) and Mycobacterium bovis BCG both in active and dormant state. Compounds 5b, 5e, 5g and 5q exhibited very good antitubercular activity. All the newly synthesized compounds 5a-t were further evaluated for antiproliferative activity against HeLa, A549 and PANC-1 cell lines using modified MTT assay and found to be noncytotoxic. On the basis of cytotoxicity and MIC values against Mycobacterium bovis BCG, selectivity index (SI) of most active compounds 5b, 5e, 5g and 5q was calculated (SI = GI(50)/MIC) in active and dormant state. Compounds 5b, 5e and 5g demonstrated SI values &amp;gt;= 10 against all three cell lines and were found to safe for advance screening. Compounds 5a-t were further screened for their antibacterial activity against four bacteria strains to assess their selectivity towards MTB. In addition, the molecular docking studies revealed the binding modes of these compounds in active site of enoyl reductase (InhA), which in turn helped to establish a structural basis of inhibition of mycobacteria. The potency, low cytotoxicity and selectivity of these compounds make them valid lead compounds for further optimization. (C) 2016 Elsevier Ltd. All rights reserved.&lt;/p&gt;</style></abstract><issue><style face="normal" font="default" size="100%">7</style></issue><custom3><style face="normal" font="default" size="100%">&lt;p&gt;Foreign&lt;/p&gt;</style></custom3><custom4><style face="normal" font="default" size="100%">2.486</style></custom4></record><record><source-app name="Biblio" version="7.x">Drupal-Biblio</source-app><ref-type>17</ref-type><contributors><authors><author><style face="normal" font="default" size="100%">Singh, Ruby</style></author><author><style face="normal" font="default" size="100%">Nawale, Laxman</style></author><author><style face="normal" font="default" size="100%">Sarkar, Dhiman</style></author><author><style face="normal" font="default" size="100%">Suresh, C. G.</style></author></authors></contributors><titles><title><style face="normal" font="default" size="100%">Two chitotriose-specific lectins show anti-angiogenesis, induces caspase-9-mediated apoptosis and early arrest of pancreatic tumor cell cycle</style></title><secondary-title><style face="normal" font="default" size="100%">Plos One</style></secondary-title></titles><dates><year><style  face="normal" font="default" size="100%">2016</style></year><pub-dates><date><style  face="normal" font="default" size="100%">JAN</style></date></pub-dates></dates><number><style face="normal" font="default" size="100%">1</style></number><publisher><style face="normal" font="default" size="100%">PUBLIC LIBRARY SCIENCE</style></publisher><pub-location><style face="normal" font="default" size="100%">1160 BATTERY STREET, STE 100, SAN FRANCISCO, CA 94111 USA</style></pub-location><volume><style face="normal" font="default" size="100%">11</style></volume><pages><style face="normal" font="default" size="100%">Article Number: e0146110</style></pages><language><style face="normal" font="default" size="100%">eng</style></language><abstract><style face="normal" font="default" size="100%">&lt;p&gt;The antiproliferative activity of two chito-specific agglutinins purified from Benincasa hispida (BhL) and Datura innoxia (DiL9) of different plant family origin was investigated on various cancer cell lines. Both lectins showed chitotriose specificity, by inhibiting lectin hemagglutinating activity. On further studies, it was revealed that these agglutinins caused remarkable concentration-dependent antiproliferative effect on human pancreatic cancerous cells but not on the normal human umbilical vein endothelial cells even at higher doses determined using MTT assay. The GI(50) values were approximately 8.4 mu g ml(-1) (0.247 mu M) and 142 mu g ml(-1) (14.8 mu M) for BhL and DiL9, respectively, against PANC-1 cells. The growth inhibitory effect of these lectins on pancreatic cancer cells were shown to be a consequence of lectin cell surface binding and triggering G(0)/G(1) arrest, mitochondrial membrane depolarization, sustained increase of the intracellular calcium release and the apoptotic signal is amplified by activation of caspases executing cell death. Interestingly, these lectins also showed anti-angiogenic activity by disrupting the endothelial tubulogenesis. Therefore, we report for the first time two chito-specific lectins specifically binding to tumor glycans; they can be considered to be a class of molecules with antitumor activity against pancreatic cancer cells mediated through caspase dependent mitochondrial apoptotic pathway.&lt;/p&gt;</style></abstract><issue><style face="normal" font="default" size="100%">1</style></issue><custom3><style face="normal" font="default" size="100%">&lt;p&gt;Foreign&lt;/p&gt;</style></custom3><custom4><style face="normal" font="default" size="100%">3.057</style></custom4></record><record><source-app name="Biblio" version="7.x">Drupal-Biblio</source-app><ref-type>17</ref-type><contributors><authors><author><style face="normal" font="default" size="100%">Nawale, Laxman</style></author><author><style face="normal" font="default" size="100%">Dubey, Parul</style></author><author><style face="normal" font="default" size="100%">Chaudhari, Bhushan</style></author><author><style face="normal" font="default" size="100%">Sarkar, Dhiman</style></author><author><style face="normal" font="default" size="100%">Prabhune, Asmita</style></author></authors></contributors><titles><title><style face="normal" font="default" size="100%">Anti-proliferative effect of novel primary cetyl alcohol derived sophorolipids against human cervical cancer cells HeLa</style></title><secondary-title><style face="normal" font="default" size="100%">Plos One</style></secondary-title></titles><dates><year><style  face="normal" font="default" size="100%">2017</style></year><pub-dates><date><style  face="normal" font="default" size="100%">APR</style></date></pub-dates></dates><volume><style face="normal" font="default" size="100%">12 </style></volume><pages><style face="normal" font="default" size="100%">e0174241</style></pages><language><style face="normal" font="default" size="100%">eng</style></language><abstract><style face="normal" font="default" size="100%">Sophorolipids (SLs) are glycolipid biosurfactants that have been shown to display anticancer activity. In the present study, we report anti-proliferative studies on purified forms of novel SLs synthesized using cetyl alcohol as the substrate (referred as SLCA) and their anticancer mechanism in human cervical cancer cells. Antiproliferative effect of column purified SLCA fractions (A, B, C, D, E and F) was examined in panel of human cancer cell lines as well as primary cells. Among these fractions, SLCA B and C significantly inhibited the survival of HeLa and HCT 116 cells without affecting the viability of normal human umbilical vein endothelial cells (HUVEC). The two fractions were identified as cetyl alcohol sophorolipids with non-hydroxylated tail differing in the degree of acetylation on sophorose head group. At an IC50 concentration SLCA B (16.32 mu g ml(-1)) and SLCA C (14.14 mu g ml(-1)) blocked the cell cycle progression of HeLa cells at G1/S phase in time-dependent manner. Moreover, SLCA B and SLCA C induced apoptosis in HeLa cells through an increase in intracellular Ca2+ leading to depolarization of mitochondrial membrane potential and increase in the caspase-3, -8 and -9 activity. All these findings suggest that these SLCAs could be explored for their chemopreventive potential in cervical cancer.</style></abstract><issue><style face="normal" font="default" size="100%">4</style></issue><work-type><style face="normal" font="default" size="100%">Article</style></work-type><custom3><style face="normal" font="default" size="100%">Foreign</style></custom3><custom4><style face="normal" font="default" size="100%">2.766</style></custom4></record><record><source-app name="Biblio" version="7.x">Drupal-Biblio</source-app><ref-type>17</ref-type><contributors><authors><author><style face="normal" font="default" size="100%">Chavan, Pramod V.</style></author><author><style face="normal" font="default" size="100%">Pandit, Kapil S.</style></author><author><style face="normal" font="default" size="100%">Desai, Uday V.</style></author><author><style face="normal" font="default" size="100%">Wadgaonkar, Prakash P.</style></author><author><style face="normal" font="default" size="100%">Nawale, Laxman</style></author><author><style face="normal" font="default" size="100%">Bhansali, Sujit</style></author><author><style face="normal" font="default" size="100%">Sarkar, Dhiman</style></author></authors></contributors><titles><title><style face="normal" font="default" size="100%">Click-chemistry-based multicomponent condensation approach for design and synthesis of spirochromene-tethered 1,2,3-triazoles as potential antitubercular agents</style></title><secondary-title><style face="normal" font="default" size="100%">Research on Chemical Intermediates</style></secondary-title></titles><dates><year><style  face="normal" font="default" size="100%">2017</style></year><pub-dates><date><style  face="normal" font="default" size="100%">OCT</style></date></pub-dates></dates><volume><style face="normal" font="default" size="100%">43</style></volume><pages><style face="normal" font="default" size="100%">5675-5690</style></pages><language><style face="normal" font="default" size="100%">eng</style></language><issue><style face="normal" font="default" size="100%">10</style></issue><work-type><style face="normal" font="default" size="100%">Article</style></work-type><custom3><style face="normal" font="default" size="100%">Foreign</style></custom3><custom4><style face="normal" font="default" size="100%">1.833</style></custom4></record><record><source-app name="Biblio" version="7.x">Drupal-Biblio</source-app><ref-type>17</ref-type><contributors><authors><author><style face="normal" font="default" size="100%">Subhedar, Dnyaneshwar D.</style></author><author><style face="normal" font="default" size="100%">Shaikh, Mubarak H.</style></author><author><style face="normal" font="default" size="100%">Shingate, Bapurao B.</style></author><author><style face="normal" font="default" size="100%">Nawale, Laxman</style></author><author><style face="normal" font="default" size="100%">Sarkar, Dhiman</style></author><author><style face="normal" font="default" size="100%">Khedkar, Vijay M.</style></author><author><style face="normal" font="default" size="100%">Khan, Firoz A. Kalam</style></author><author><style face="normal" font="default" size="100%">Sangshetti, Jaiprakash N.</style></author></authors></contributors><titles><title><style face="normal" font="default" size="100%">Quinolidene-rhodanine conjugates: facile synthesis and biological evaluation</style></title><secondary-title><style face="normal" font="default" size="100%">European Journal of Medicinal Chemistry</style></secondary-title></titles><dates><year><style  face="normal" font="default" size="100%">2017</style></year><pub-dates><date><style  face="normal" font="default" size="100%">JAN</style></date></pub-dates></dates><volume><style face="normal" font="default" size="100%">125</style></volume><pages><style face="normal" font="default" size="100%">385–399</style></pages><language><style face="normal" font="default" size="100%">eng</style></language><abstract><style face="normal" font="default" size="100%">&lt;p&gt;A series of rhodanine incorporated quinoline derivatives were efficiently synthesized using reusable DBU acetate as ionic liquid and evaluated for their in vitro antitubercular activity against Mycobacterium tuberculosis H37Ra (MTB) (ATCC 25177) and Mycobacterium bovis BCG (ATCC 35743) both in active and dormant state. Compounds 3e, 3f, 3g, 3h and 3i exhibited very good antitubercular activity. The active compounds were studied for cytotoxicity against HUVEC, THP-1, macrophages, A549, PANC-1 and HeLa cell lines using modified MTT assay and were found to be noncytotoxic. Inactivity of all these compounds against Gram positive and Gram negative bacteria indicates their specificity towards the MTB. Further, the synthesized compounds have been screened for their in vitro antifungal activity. In addition, the molecular docking studies revealed the binding modes of these compounds in active site of Zmp1 enzyme, which in turn helped to establish a structural basis of inhibition of mycobacteria. The results of present study clearly indicate the identification of some novel, selective and specific inhibitors against MTB that can be explored further for potential antitubercular drug.&lt;/p&gt;</style></abstract><work-type><style face="normal" font="default" size="100%">Article</style></work-type><custom3><style face="normal" font="default" size="100%">&lt;p&gt;Foreign&lt;/p&gt;</style></custom3><custom4><style face="normal" font="default" size="100%">&lt;p&gt;3.902&lt;/p&gt;</style></custom4></record><record><source-app name="Biblio" version="7.x">Drupal-Biblio</source-app><ref-type>17</ref-type><contributors><authors><author><style face="normal" font="default" size="100%">Abhale, Yogita K.</style></author><author><style face="normal" font="default" size="100%">Sasane, Amit V.</style></author><author><style face="normal" font="default" size="100%">Chavan, Abhijit P.</style></author><author><style face="normal" font="default" size="100%">Shekh, Saddam Husen</style></author><author><style face="normal" font="default" size="100%">Deshmukh, Keshav K.</style></author><author><style face="normal" font="default" size="100%">Bhansali, Sujit</style></author><author><style face="normal" font="default" size="100%">Nawale, Laxman</style></author><author><style face="normal" font="default" size="100%">Sarkar, Dhiman</style></author><author><style face="normal" font="default" size="100%">Mhaske, Pravin C.</style></author></authors></contributors><titles><title><style face="normal" font="default" size="100%">Synthesis and antimycobacterial screening of new thiazolyl-oxazole derivatives</style></title><secondary-title><style face="normal" font="default" size="100%">European Journal of Medicinal Chemistry</style></secondary-title></titles><dates><year><style  face="normal" font="default" size="100%">2017</style></year><pub-dates><date><style  face="normal" font="default" size="100%">MAY</style></date></pub-dates></dates><volume><style face="normal" font="default" size="100%">132</style></volume><pages><style face="normal" font="default" size="100%">333-340</style></pages><language><style face="normal" font="default" size="100%">eng</style></language><abstract><style face="normal" font="default" size="100%">&lt;p&gt;In the present study a series of 4-methyl-2-aryl-5-(2-aryl/benzyl thiazol-4-yl) oxazole (4a-v) have been synthesized and evaluated for their preliminary antitubercular, antimicrobial and cytotoxicity activity. Among all the synthesized compounds, 4v reported comparable activity against dormant M. tuberculosis H37Ra and M. bovis BCG strains with respect to standard drug rifampicin. The active compounds from the antitubercular study were further tested for anti-proliferative activity against HeLa, A549 and PANC-1 cell lines using MU assay and showed no significant cytotoxic activity at the maximum concentration evaluated. Further, the synthesized compounds were found to have potential antibacterial activities with MIC range of 2.1-26.8 mu g/mL. High potency, lower cytotoxicity and promising antimycobacterial activity suggested that these compounds could serve as good leads for further optimisation and development. (C) 2017 Elsevier Masson SAS. All rights reserved.&lt;/p&gt;</style></abstract><work-type><style face="normal" font="default" size="100%">Article</style></work-type><custom3><style face="normal" font="default" size="100%">Foreign</style></custom3><custom4><style face="normal" font="default" size="100%">&lt;p&gt;3.902&lt;/p&gt;</style></custom4></record><record><source-app name="Biblio" version="7.x">Drupal-Biblio</source-app><ref-type>17</ref-type><contributors><authors><author><style face="normal" font="default" size="100%">Rode, Navnath D.</style></author><author><style face="normal" font="default" size="100%">Sonawane, Amol D.</style></author><author><style face="normal" font="default" size="100%">Nawale, Laxman</style></author><author><style face="normal" font="default" size="100%">Khedkar, Vijay M.</style></author><author><style face="normal" font="default" size="100%">Joshi, Ramesh A.</style></author><author><style face="normal" font="default" size="100%">Likhite, Anjali P.</style></author><author><style face="normal" font="default" size="100%">Sarkar, Dhiman</style></author><author><style face="normal" font="default" size="100%">Joshi, Rohini R.</style></author></authors></contributors><titles><title><style face="normal" font="default" size="100%">Synthesis, biological evaluation, and molecular docking studies of novel 3-aryl-5-(alkyl-thio)-1H-1,2,4-triazoles derivatives targeting Mycobacterium tuberculosis</style></title><secondary-title><style face="normal" font="default" size="100%">Chemical Biology &amp; Drug Design</style></secondary-title></titles><dates><year><style  face="normal" font="default" size="100%">2017</style></year><pub-dates><date><style  face="normal" font="default" size="100%">DEC</style></date></pub-dates></dates><volume><style face="normal" font="default" size="100%">90</style></volume><pages><style face="normal" font="default" size="100%">1206-1214</style></pages><language><style face="normal" font="default" size="100%">eng</style></language><abstract><style face="normal" font="default" size="100%">A small library of new 3-aryl-5-(alkyl-thio)-1H-1,2,4-triazoles was synthesized and screened for the antimycobacterial potency against Mycobacterium tuberculosis H37Ra strain and Mycobacterium bovis BCG both in active and dormant stage. Among the synthesized library, 25 compounds exhibited promising anti-TB activity in the range of IC(50)0.03-5.88g/ml for dormant stage and 20 compounds in the range of 0.03-6.96g/ml for active stage. Their lower toxicity (&gt;100g/ml) and higher selectivity (SI=&gt;10) against all cancer cell lines screened make them interesting compounds with potential antimycobacterial effects. Furthermore, to rationalize the observed biological activity data and to establish a structural basis for inhibition of M.tuberculosis, the molecular docking study was carried out against a potential target MTB CYP121 which revealed a significant correlation between the binding score and biological activity for these compounds. Cytotoxicity and in vivo pharmacokinetic studies suggested that 1,2,4-triazole analogues have an acceptable safety index, in vivo stability and bio-availability.</style></abstract><issue><style face="normal" font="default" size="100%">6</style></issue><work-type><style face="normal" font="default" size="100%">Article</style></work-type><custom3><style face="normal" font="default" size="100%">Foreign</style></custom3><custom4><style face="normal" font="default" size="100%">2.802</style></custom4></record><record><source-app name="Biblio" version="7.x">Drupal-Biblio</source-app><ref-type>17</ref-type><contributors><authors><author><style face="normal" font="default" size="100%">Shaikh, Mubarak H.</style></author><author><style face="normal" font="default" size="100%">Subhedar, Dnyaneshwar D.</style></author><author><style face="normal" font="default" size="100%">Khan, Firoz A. Kalam</style></author><author><style face="normal" font="default" size="100%">Sangshetti, Jaiprakash N.</style></author><author><style face="normal" font="default" size="100%">Nawale, Laxman</style></author><author><style face="normal" font="default" size="100%">Arkile, Manisha A.</style></author><author><style face="normal" font="default" size="100%">Sarkar, Dhiman</style></author><author><style face="normal" font="default" size="100%">Shingate, Bapurao B.</style></author></authors></contributors><titles><title><style face="normal" font="default" size="100%">Synthesis of novel triazole-incorporated isatin derivatives as antifungal, antitubercular, and antioxidant agents and molecular docking study</style></title><secondary-title><style face="normal" font="default" size="100%">Journal of Heterocyclic Chemistry</style></secondary-title></titles><dates><year><style  face="normal" font="default" size="100%">2017</style></year><pub-dates><date><style  face="normal" font="default" size="100%">JAN</style></date></pub-dates></dates><volume><style face="normal" font="default" size="100%">54</style></volume><language><style face="normal" font="default" size="100%">eng</style></language><abstract><style face="normal" font="default" size="100%">&lt;p&gt;A library of 1,2,3-triazoles efficiently prepared via click chemistry and evaluated for their antifungal, antitubercular, antioxidant, cytotoxicity, molecular docking and ADME prediction.&lt;/p&gt;</style></abstract><issue><style face="normal" font="default" size="100%">413</style></issue><work-type><style face="normal" font="default" size="100%">Article</style></work-type><custom3><style face="normal" font="default" size="100%">&lt;p&gt;Foreign&lt;/p&gt;</style></custom3><custom4><style face="normal" font="default" size="100%">&lt;p&gt;0.685&lt;/p&gt;</style></custom4></record><record><source-app name="Biblio" version="7.x">Drupal-Biblio</source-app><ref-type>17</ref-type><contributors><authors><author><style face="normal" font="default" size="100%">Bhosle, Govind S.</style></author><author><style face="normal" font="default" size="100%">Nawale, Laxman</style></author><author><style face="normal" font="default" size="100%">Yeware, Amar M.</style></author><author><style face="normal" font="default" size="100%">Sarkar, Dhiman</style></author><author><style face="normal" font="default" size="100%">Fernandes, Moneesha</style></author></authors></contributors><titles><title><style face="normal" font="default" size="100%">Antibacterial and anti-TB tat-peptidomimetics with improved efficacy and half-life</style></title><secondary-title><style face="normal" font="default" size="100%">European Journal of Medicinal Chemistry</style></secondary-title></titles><dates><year><style  face="normal" font="default" size="100%">2018</style></year><pub-dates><date><style  face="normal" font="default" size="100%">MAY</style></date></pub-dates></dates><volume><style face="normal" font="default" size="100%">152</style></volume><pages><style face="normal" font="default" size="100%">358-369</style></pages><language><style face="normal" font="default" size="100%">eng</style></language><abstract><style face="normal" font="default" size="100%">Non-natural antimicrobial peptides are ideal as next-generation antibiotics because of their ability to circumvent the problems of drug resistance and in vivo instability. We report novel all-alpha- and alpha,gamma-mixed Tat peptide analogues as potential antibacterial and anti-TB agents. These peptides have broad spectrum antibacterial activities against Gram-positive (MICs 0.61 +/- 0.03 to 1.35 +/- 0.21 mu M with the peptide gamma TatM4) and Gram-negative (MICs 0.71 +/- 0.005 to 1.26 +/- 0.02 M with gamma TatM4) bacteria and are also effective against active and dormant forms of Mycobacterium tuberculosis, including strains that are resistant to rifampicin and isoniazid. The introduction of the non-natural amino acids of the study in the Tat peptide analogues results in increased resistance to degradation by proteolysis, significantly increasing their half-life. The peptides appear to inhibit bacteria by a membrane disruption mechanism, and have only a low cytotoxic effect on mammalian cells. (C) 2018 Elsevier Masson SAS. All rights reserved.</style></abstract><custom3><style face="normal" font="default" size="100%">Foreign</style></custom3><custom4><style face="normal" font="default" size="100%">4.519</style></custom4></record><record><source-app name="Biblio" version="7.x">Drupal-Biblio</source-app><ref-type>17</ref-type><contributors><authors><author><style face="normal" font="default" size="100%">Gholap, Somnath</style></author><author><style face="normal" font="default" size="100%">Tambe, Macchindra</style></author><author><style face="normal" font="default" size="100%">Nawale, Laxman</style></author><author><style face="normal" font="default" size="100%">Sarkar, Dhiman</style></author><author><style face="normal" font="default" size="100%">Sangshetti, Jaiprakash</style></author><author><style face="normal" font="default" size="100%">Damale, Manoj</style></author></authors></contributors><titles><title><style face="normal" font="default" size="100%">Design, synthesis, and pharmacological evaluation of fluorinated azoles as anti-tubercular agents</style></title><secondary-title><style face="normal" font="default" size="100%">Archiv Der Pharmazie</style></secondary-title></titles><keywords><keyword><style  face="normal" font="default" size="100%">1</style></keyword><keyword><style  face="normal" font="default" size="100%">2</style></keyword><keyword><style  face="normal" font="default" size="100%">2-dimethyl-2</style></keyword><keyword><style  face="normal" font="default" size="100%">3</style></keyword><keyword><style  face="normal" font="default" size="100%">3-dihydrobenzofuran</style></keyword><keyword><style  face="normal" font="default" size="100%">4-Oxadiazole</style></keyword><keyword><style  face="normal" font="default" size="100%">anti-tubercular agents</style></keyword><keyword><style  face="normal" font="default" size="100%">Cytotoxicity</style></keyword><keyword><style  face="normal" font="default" size="100%">Molecular docking</style></keyword></keywords><dates><year><style  face="normal" font="default" size="100%">2018</style></year><pub-dates><date><style  face="normal" font="default" size="100%">FEB</style></date></pub-dates></dates><volume><style face="normal" font="default" size="100%">351</style></volume><pages><style face="normal" font="default" size="100%">e1700294</style></pages><language><style face="normal" font="default" size="100%">eng</style></language><abstract><style face="normal" font="default" size="100%">&lt;p&gt;Design, synthesis, and biological screening of 2,2-dimethyl-2,3-dihydrobenzofuran tethered 1,3,4-oxadiazole derivatives as anti-tubercular agents were described. The synthesis of the target compounds was conducted by a series of reaction schemes. All the synthesized compounds were characterized by IR, H-1 NMR, C-13 NMR, and mass spectrometry. The therapeutic potential of the synthesized compounds was confirmed by molecular docking studies. Among the synthesized compounds, 12a, 12c, 12d, 12e, 12g, and 12j were found to be more active against non-replicating than against replicating cultures of Mycobacterium tuberculosis H37Ra ex vivo and in vitro. These compounds exhibit minimum inhibitory concentration (MIC) values in the range of 2.31-23.91g/mL. The cytotoxicity study was conducted against the cell lines THP-1, A549 and PANC-1, and the compounds were observed to be non-toxic to host cells. Molecular docking was conducted with InhA (FabI/ENR) and suggested the antimycobacterial potential of the synthesized compounds. The investigation presented here was found to be adventitious for the development of new therapeutic agents against Mycobacterium infection.&lt;/p&gt;</style></abstract><issue><style face="normal" font="default" size="100%">2</style></issue><work-type><style face="normal" font="default" size="100%">Article</style></work-type><custom3><style face="normal" font="default" size="100%">Foreign</style></custom3><custom4><style face="normal" font="default" size="100%">1.994</style></custom4></record><record><source-app name="Biblio" version="7.x">Drupal-Biblio</source-app><ref-type>17</ref-type><contributors><authors><author><style face="normal" font="default" size="100%">Shaikh, Mubarak H.</style></author><author><style face="normal" font="default" size="100%">Subhedar, Dnyaneshwar</style></author><author><style face="normal" font="default" size="100%">Nawale, Laxman</style></author><author><style face="normal" font="default" size="100%">Sarkar, Dhiman</style></author><author><style face="normal" font="default" size="100%">Khan, Firoz A. Kalam</style></author><author><style face="normal" font="default" size="100%">Sangshetti, Jaiprakash</style></author><author><style face="normal" font="default" size="100%">Shingate, Bapurao B.</style></author></authors></contributors><titles><title><style face="normal" font="default" size="100%">Novel benzylidenehydrazide-1,2,3-triazole conjugates as antitubercular agents: synthesis and molecular docking</style></title><secondary-title><style face="normal" font="default" size="100%">Mini Reviews in Medicinal Chemistry</style></secondary-title></titles><dates><year><style  face="normal" font="default" size="100%">2018</style></year><pub-dates><date><style  face="normal" font="default" size="100%">JUL</style></date></pub-dates></dates><volume><style face="normal" font="default" size="100%">18</style></volume><language><style face="normal" font="default" size="100%">eng</style></language><abstract><style face="normal" font="default" size="100%">Novel 1,2,3-triazole based benzylidenehydrazide derivatives were synthesized and evaluated for antitubercular activity against Mycobacterium tuberculosis (MTB) H37Ra, M. bovis BCG and cytotoxic activity. Most of the derivatives exhibited promising in vitro potency against MTB characterized by lower MIC values. Among all the synthesized derivatives, compound 6a and 6j were the most active against active and dormant MTB H37Ra, respectively. Compound 6d was significantly active against dormant and active M. bovis BCG. The structure activity relationship has been explored on the basis of anti-tubercular activity data. The active compounds were also tested against THP-1, A549 and Panc-1 cell lines and showed no significant cytotoxicity. Further, the synthesized compounds were found to have potential antioxidant with IC50 range = 11.19-56.64 μg/mL. The molecular docking study of synthesized compounds was performed against DprE1 enzyme of MTB to understand the binding interactions. Moreover, synthesized compounds were also analysed for ADME properties and from all the experimental results, the potency of compounds indicate that, this series considered as starting point for the developement of novel and more potent anti-tubercular agents in future.</style></abstract><custom3><style face="normal" font="default" size="100%">Foreign</style></custom3><custom4><style face="normal" font="default" size="100%">2.661</style></custom4></record><record><source-app name="Biblio" version="7.x">Drupal-Biblio</source-app><ref-type>17</ref-type><contributors><authors><author><style face="normal" font="default" size="100%">Shinde, Vikas</style></author><author><style face="normal" font="default" size="100%">Mahulikar, Pramod</style></author><author><style face="normal" font="default" size="100%">Mhaske, Pravin C.</style></author><author><style face="normal" font="default" size="100%">Nawale, Laxman</style></author><author><style face="normal" font="default" size="100%">Sarkar, Dhiman</style></author></authors></contributors><titles><title><style face="normal" font="default" size="100%">Synthesis and biological evaluation of new 2-aryl-4-((4-aryl-1H-1,2,3-triazol-1-yl)methyl)thiazole derivatives</style></title><secondary-title><style face="normal" font="default" size="100%">Research on Chemical Intermediates</style></secondary-title></titles><keywords><keyword><style  face="normal" font="default" size="100%">1</style></keyword><keyword><style  face="normal" font="default" size="100%">2</style></keyword><keyword><style  face="normal" font="default" size="100%">3-Triazole</style></keyword><keyword><style  face="normal" font="default" size="100%">antibacterial activity</style></keyword><keyword><style  face="normal" font="default" size="100%">Antitubercular activity</style></keyword><keyword><style  face="normal" font="default" size="100%">Thiazole</style></keyword></keywords><dates><year><style  face="normal" font="default" size="100%">2018</style></year><pub-dates><date><style  face="normal" font="default" size="100%">FEB</style></date></pub-dates></dates><volume><style face="normal" font="default" size="100%">44</style></volume><pages><style face="normal" font="default" size="100%">1247-1260</style></pages><language><style face="normal" font="default" size="100%">eng</style></language><abstract><style face="normal" font="default" size="100%">&lt;p&gt;A series of 2-aryl-4-((4-aryl-1H-1,2,3-triazol-1-yl)methyl)thiazole derivatives (8a-p) have been synthesized. The structure of the newly synthesized compounds was determined by spectral analysis. The title compounds were screened for their preliminary antitubercular activity against Mycobacterium tuberculosis H37Ra (MTB, ATCC 25177) and Mycobacterium bovis BCG (BCG, ATCC 35743). Further, the synthesized compounds were screened for antimicrobial activity against standard Gram-negative bacteria Escherichia coli (NCIM 2576) and Pseudomonas flurescence (NCIM 2059) and Gram-positive bacteria Staphylococcus aureus (NCIM 2602) and Bacillus subtilis (NCIM 2162). Among all the synthesized compounds, 8a-c, f-h, m exhibited good activity against dormant M. bovis BCG strain. Compounds 8h, j exhibited good activity against all tested bacterial strains. All active compounds were screened for cytotoxicity and found inactive. Their high potency and promising antimycobacterial activity suggest that these compounds could serve as good leads for further optimization and development.&lt;/p&gt;</style></abstract><issue><style face="normal" font="default" size="100%">2</style></issue><work-type><style face="normal" font="default" size="100%">Article</style></work-type><custom3><style face="normal" font="default" size="100%">Foreign</style></custom3><custom4><style face="normal" font="default" size="100%">1.369</style></custom4></record><record><source-app name="Biblio" version="7.x">Drupal-Biblio</source-app><ref-type>17</ref-type><contributors><authors><author><style face="normal" font="default" size="100%">Takate, Sushma J.</style></author><author><style face="normal" font="default" size="100%">Shinde, Abhijit D.</style></author><author><style face="normal" font="default" size="100%">Karale, Bhausaheb K.</style></author><author><style face="normal" font="default" size="100%">Akolkar, Hemant</style></author><author><style face="normal" font="default" size="100%">Nawale, Laxman</style></author><author><style face="normal" font="default" size="100%">Sarkar, Dhiman</style></author><author><style face="normal" font="default" size="100%">Mhaske, Pravin C.</style></author></authors></contributors><titles><title><style face="normal" font="default" size="100%">Thiazolyl-pyrazole derivatives as potential antimycobacterial agents</style></title><secondary-title><style face="normal" font="default" size="100%">Bioorganic &amp; Medicinal Chemistry Letters</style></secondary-title></titles><keywords><keyword><style  face="normal" font="default" size="100%">antimycobacterial activity</style></keyword><keyword><style  face="normal" font="default" size="100%">Cytotoxicity</style></keyword><keyword><style  face="normal" font="default" size="100%">Pyrazole</style></keyword><keyword><style  face="normal" font="default" size="100%">thiazoles</style></keyword></keywords><dates><year><style  face="normal" font="default" size="100%">2019</style></year><pub-dates><date><style  face="normal" font="default" size="100%">MAY</style></date></pub-dates></dates><volume><style face="normal" font="default" size="100%">29</style></volume><pages><style face="normal" font="default" size="100%">1199-1202</style></pages><language><style face="normal" font="default" size="100%">eng</style></language><abstract><style face="normal" font="default" size="100%">&lt;p&gt;Mycobacterium tuberculosis (Mtb) is an obligate aerobe that is capable of long-term persistence under conditions of low oxygen tension. A series of thiazolyl-pyrazole derivatives (6a-f, 7a-f, 8c, 8e) were screened for antimycobacterial activity against dormant M. tuberculosis H37Ra (D-MTB) and M. bovis BCG (D-BCG). Nine thiazolyl- pyrazole analogs, 6c, 6e, 7a, 7b, 7c, 7e, 7f, 8c and 8e exhibited promissing minimum inhibitory concentration (MIC) values (0.20-28.25 mu g/mL) against D-MTB and D-BCG strains of Mtb. Importantly, six compounds (7a, 7b, 7e, 7f, 8c and 8e) exhibited excellent antimycobacterial activity and low cytotoxicity at the maximum evaluated concentration of &amp;gt; 250 mu g/mL. Finally, the promising antimycobacterial activity and lower cytotoxicity profile suggested that, these compounds could be further subjected for optimization and development as a lead, which could have the potential to treat tuberculosis.&lt;/p&gt;</style></abstract><issue><style face="normal" font="default" size="100%">10</style></issue><work-type><style face="normal" font="default" size="100%">Article</style></work-type><custom3><style face="normal" font="default" size="100%">Foreign</style></custom3><custom4><style face="normal" font="default" size="100%">2.442</style></custom4></record><record><source-app name="Biblio" version="7.x">Drupal-Biblio</source-app><ref-type>17</ref-type><contributors><authors><author><style face="normal" font="default" size="100%">Abhale, Yogita K.</style></author><author><style face="normal" font="default" size="100%">Shinde, Abhijit</style></author><author><style face="normal" font="default" size="100%">Shelke, Monika</style></author><author><style face="normal" font="default" size="100%">Nawale, Laxman</style></author><author><style face="normal" font="default" size="100%">Sarkar, Dhiman</style></author><author><style face="normal" font="default" size="100%">Mhaske, Pravin C.</style></author></authors></contributors><titles><title><style face="normal" font="default" size="100%">Synthesis of new 2-(thiazol-4-yl)thiazolidin-4-one derivatives as potential anti-mycobacterial agents</style></title><secondary-title><style face="normal" font="default" size="100%">Bioorganic Chemistry</style></secondary-title></titles><keywords><keyword><style  face="normal" font="default" size="100%">Cytotoxicity</style></keyword><keyword><style  face="normal" font="default" size="100%">Mycobacterium tuberculosis</style></keyword><keyword><style  face="normal" font="default" size="100%">Thiazole</style></keyword><keyword><style  face="normal" font="default" size="100%">Thiazolidin-4-one</style></keyword></keywords><dates><year><style  face="normal" font="default" size="100%">2021</style></year><pub-dates><date><style  face="normal" font="default" size="100%">OCT</style></date></pub-dates></dates><volume><style face="normal" font="default" size="100%">115</style></volume><pages><style face="normal" font="default" size="100%">105192</style></pages><language><style face="normal" font="default" size="100%">eng</style></language><abstract><style face="normal" font="default" size="100%">To search for potent antimycobacterial lead compounds, a new series of 3-substituted phenyl-2-(2-(substituted phenyl)thiazol-4-yl) thiazolidin-4-one (5a-t) derivatives have been synthesized by the condensation of 2 substituted phenyl thiazole-4-carbaldehyde with aromatic amine followed by cyclocondensation with thioglycolic acid. The structure of the newly synthesized 2-(thiazol-4-yl)thiazolidin-4-one derivatives were characterized by the spectroscopic analysis. The synthesized compounds were screened for antimycobacterial activity against Mycobacterium tuberculosis H37Ra (MTB) (ATCC 25177) and Mycobacterium bovis BCG (BCG, ATCC 35743). Most of the 2-(thiazol-4-yl)thiazolidin-4-one derivatives showed good to excellent antimycobacterial activity against both the Mtb strains. Nine derivatives 5c, 5g, 5j, 5m, 5n, 5o, 5p, 5s, and 5t showed excellent activity against M. bovis BCG with MIC 4.43 to 24.04 mu M were further evaluated for the cytotoxicity activity against HeLa A549, and HCT-116 cell lines and showed no significant cytotoxic activity at the maximum concentration evaluated. The potential antimycobacterial activities enforced that the thiazolyl-thiazolidin-4-one derivatives could lead to compounds that could treat tuberculosis.</style></abstract><work-type><style face="normal" font="default" size="100%">Article</style></work-type><custom3><style face="normal" font="default" size="100%">Foreign</style></custom3><custom4><style face="normal" font="default" size="100%">5.275</style></custom4></record></records></xml>