<?xml version="1.0" encoding="UTF-8"?><xml><records><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>17</ref-type><contributors><authors><author><style face="normal" font="default" size="100%">Gadekar, Pradip K.</style></author><author><style face="normal" font="default" size="100%">Roychowdhury, Abhijit</style></author><author><style face="normal" font="default" size="100%">Kharkar, Prashant S.</style></author><author><style face="normal" font="default" size="100%">Khedkar, Vijay M.</style></author><author><style face="normal" font="default" size="100%">Arkile, Manisha A.</style></author><author><style face="normal" font="default" size="100%">Manek, Hardik</style></author><author><style face="normal" font="default" size="100%">Sarkar, Dhiman</style></author><author><style face="normal" font="default" size="100%">Sharma, Rajiv</style></author><author><style face="normal" font="default" size="100%">Vijayakumar, V.</style></author><author><style face="normal" font="default" size="100%">Sarveswari, S.</style></author></authors></contributors><titles><title><style face="normal" font="default" size="100%">Design, synthesis and biological evaluation of novel azaspiro analogs of linezolid as antibacterial and antitubercular agents</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%">2016</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%">122</style></volume><pages><style face="normal" font="default" size="100%">475-487</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 design, synthesis and antimicrobial evaluation of a novel series of azaspiro analogues of linezolid (1) have been described. Linezolid comprises of a morpholine ring which is known for its metabolism related liabilities. Therefore, the key modification made in the linezolid structure was the replacement of morpholine moiety with its bioisostere, 2-oxa-6-azaspiro[3.3]heptane. Furthermore, the replacement of N-acetyl terminal of 1 with various aromatic or aliphatic functionalities was carried out. The title compounds were evaluated against a panel of Gram-positive and Gram-negative bacteria and Mycobacterium tuberculosis. Subsequent structure-activity relationship (SAR) studies identified several compounds with mixed antibacterial and antitubercular profiles. Compound 22 (IC50 0.72, 0.51, 0.88, 0.49 mu g/mL for Escherichia coli, Pseudomonas aeruginosa, Staphylococcus aureus, Bacillus subtilis, respectively) exhibited similar antibacterial profile as I. The N-acetyl derivative 18 was similar to 1 in antitubercular profile. Thus, the present study successfully demonstrated the use of azaspiro substructure in the medicinal chemistry of antibacterial and antitubercular agents. (C) 2016 Elsevier Masson SAS. All rights reserved.&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%">3.902</style></custom4></record></records></xml>