01753nas a2200229 4500008004100000245008300041210006900124260000800193300001200201490000800213520098800221100002301209700002101232700002401253700002501277700002501302700002001327700001901347700001901366700002301385856011501408 2017 eng d00aSynthesis and antimycobacterial screening of new thiazolyl-oxazole derivatives0 aSynthesis and antimycobacterial screening of new thiazolyloxazol cMAY a333-3400 v1323 a

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.

1 aAbhale, Yogita, K.1 aSasane, Amit, V.1 aChavan, Abhijit, P.1 aShekh, Saddam, Husen1 aDeshmukh, Keshav, K.1 aBhansali, Sujit1 aNawale, Laxman1 aSarkar, Dhiman1 aMhaske, Pravin, C. uhttps://library.ncl.res.in/content/synthesis-and-antimycobacterial-screening-new-thiazolyl-oxazole-derivatives02342nas a2200193 4500008004100000245013600041210006900177260000800246520155600254100002301810700002401833700002501857700002301882700001901905700002801924700002501952700002301977856014802000 2017 eng d00aSynthesis, antimycobacterial screening and molecular docking studies of 4-aryl-4′-methyl-2′-aryl-2,5′-bisthiazole derivatives0 aSynthesis antimycobacterial screening and molecular docking stud cJUL3 aA series of 4-aryl-4′-methyl-2′-aryl-2,5′-bisthia- zole derivatives (5a–o) were synthesized and screened for inhibitory activity against Mycobacterium tuberculosis H37Ra (ATCC 25177) and Mycobacterium bovis BCG (ATCC 35743) strains. Five lead compounds (5e, 5f, 5g, 5h, and 5o) were further confirmed from their dose dependent effect against MTB and Bovine–Calmette–Guerin. The most promising compounds 5f (MIC90: 11.32 μg/mL), 5h (MIC90: 11.59 μg/mL), and 5o (MIC90: 23.64 μg/mL) showed strong antitubercular activity against dormant MTB and BCG as well as almost insignificant cytotoxicity up to 100μg/mL against HeLa, A549, and PANC-1 human cancer cell lines. Further, the synthesized compounds were found to have potential antibacterial activity against Gram-negative bac- teria, Escherichia coli, Pseudomonas flurescence and Gram- positive bacteria, Staphylococcus aureus, Bacillus subtilis. Most of the synthesized compounds showed moderateactivity against fungal strain Candida albicans. Molecular docking studies of these compounds showed significant interactions with crystal structure of the cytochrome P45014α-sterol demethylase (CYP51) PDB ID: 1E9X. Hydrogen bond interactions with SER261 and VAL395 are important interactions for selective inhibition of designed inhibitors. Compounds 5f, 5h, and 5o showed significant interactions with 1E9X. All the experimental results promote us to consider this series as a starting point for the devel- opment of novel, selective and more potent antitubercular agents in the future.1 aAbhale, Yogita, K.1 aShinde, Abhijit, D.1 aDeshmukh, Keshav, K.1 aNawale, Laxman, U.1 aSarkar, Dhiman1 aChoudhari, Prafulla, B.1 aKumbhar, Santosh, S.1 aMhaske, Pravin, C. uhttps://library.ncl.res.in/content/synthesis-antimycobacterial-screening-and-molecular-docking-studies-4-aryl-4%E2%80%B2-methyl-2%E2%80%B2-aryl02099nas a2200253 4500008004100000022001400041245010600055210006900161260000800230300001100238490000800249520125600257653001701513653003101530653001301561653002201574100002301596700002001619700001901639700001901658700001901677700002301696856012601719 2021 eng d a0045-206800aSynthesis of new 2-(thiazol-4-yl)thiazolidin-4-one derivatives as potential anti-mycobacterial agents0 aSynthesis of new 2thiazol4ylthiazolidin4one derivatives as poten cOCT a1051920 v1153 aTo 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.10aCytotoxicity10aMycobacterium tuberculosis10aThiazole10aThiazolidin-4-one1 aAbhale, Yogita, K.1 aShinde, Abhijit1 aShelke, Monika1 aNawale, Laxman1 aSarkar, Dhiman1 aMhaske, Pravin, C. uhttps://library.ncl.res.in/content/synthesis-new-2-thiazol-4-ylthiazolidin-4-one-derivatives-potential-anti-mycobacterial01555nas a2200253 4500008004100000022001400041245011200055210006900167520065400236653001500890653002700905653001700932653003100949653001400980653001300994100002701007700002301034700002401057700002401081700002301105700001901128700002201147856013201169 2022 eng d a1551-700400aSynthesis and antimycobacterial screening of a novel series of alpha-amino acids containing thiazole linker0 aSynthesis and antimycobacterial screening of a novel series of a3 a

A small focused library of uncommon (S)-2-amino-3-(4-(((4-methyl-2-arylthiazol-5-yl)methyl)amino)phenyl) propanoic acid (5a-e) and (S)-2-amino-3-(4-(((2-arylthiazol-4-yl)methyl)amino)phenyl)propanoic acid (9a-d) derivatives have been efficiently synthesized by employing molecular simplification. The title compounds were screened for inhibitory activity against Mycobacterium tuberculosis H37Ra (MTB) and Mycobacterium bovis (BCG) strains. The cytotoxicity study was conducted against primary Human Umbilical Vein Endothelial Cells (HUVECs), on two different human tumor cells HeLa, and HCT 116 and was observed non-toxic to host cells.

10aAmino acid10aantibacterial activity10aCytotoxicity10aMycobacterium tuberculosis10asynthesis10aThiazole1 aNalawade, Jitendra, L.1 aMhaske, Pravin, C.1 aShinde, Abhijit, D.1 aChavan, Abhijit, P.1 aAbhale, Yogita, K.1 aSarkar, Dhiman1 aBobade, Vivek, D. uhttps://library.ncl.res.in/content/synthesis-and-antimycobacterial-screening-novel-series-alpha-amino-acids-containing-thiazole02255nas a2200289 4500008004100000022001400041245013300055210006900188260000800257300001400265490000700279520128400286653001701570653002701587653003101614653001301645653001301658100002601671700002301697700002001720700002001740700002201760700002401782700001901806700002301825856011701848 2022 eng d a1040-663800aSynthesis of new thiazole and pyrazole clubbed 1,2,3-triazol derivatives as potential antimycobacterial and antibacterial agents0 aSynthesis of new thiazole and pyrazole clubbed 123triazol deriva cJUL a3216-32370 v423 a

New series of 4-methyl-2-(4-substituted phenyl)-5-(4-((4-(4-substituted phenyl)-1H-1,2,3-triazol-1-yl)methyl)-1-phenyl-1H-pyrazol-3-yl)thiazole, 6a-t and 4-(1,3-diphenyl-1H-pyrazol-4-yl)-1-((1,3-diphenyl-1H-pyrazol-4-yl)methyl )-1H-1,2,3-triazole, 11a-o derivatives have been synthesized by applying copper-catalyzed [3 + 2] cycloaddition reaction. The newly synthesized 1,3-thiazolyl-pyrazolyl-1,2,3-triazole (6a-t) and bis-pyrazolyl-1,2,3-triazole (11a-o) derivatives were screened for in vitro antimycobacterial activity against M. Tuberculosis H37Ra dormant and active and antibacterial activity against four pathogenic bacteria, E. coli (NCIM 2576), P. flurescence (NCIM 2059), S. aureus (NCIM 2602) and B. subtilis (NCIM 2162). Compounds 6a, 6f, 6j, 11e and 11m showed good activity against M tuberculosis H37Ra Active strain, also compounds 6g, 6h, 11f, 11n and 11o showed good activity against M tuberculosis H37Ra Dormant strain. Compounds 6b, 6i, 6l, 6o, 6r, 11k, 11l and 11m showed good activity against B. subtilis with IC50 1.99-2.96 mu g/mL. The antibacterial activity of thiazolyl-pyrazolyl-1,2,3-triazole and bis-pyrazolyl-1,2,3-triazole derivatives suggested that, these derivatives could lead to new compounds for treatment against bacterial infection.

10a123-Triazole10aantibacterial activity10aantimycobacterial activity10aPyrazole10aThiazole1 aJagadale, Shivaji, M.1 aAbhale, Yogita, K.1 aPawar, Hari, R.1 aShinde, Abhijit1 aBobade, Vivek, D.1 aChavan, Abhijit, P.1 aSarkar, Dhiman1 aMhaske, Pravin, C. uhttps://library.ncl.res.in/content/synthesis-new-thiazole-and-pyrazole-clubbed-123-triazol-derivatives-potential02258nas a2200265 4500008004100000022001400041245016900055210006900224260000900293300001200302490000700314520130000321653002001621653002701641653002401668653002201692100002301714700002001737700002301757700002201780700002201802700001901824700002301843856012601866 2024 eng d a1040-663800aSynthesis and antimicrobial evaluation of novel 2'-aryl-4-aryl-2,4'-Bisthiazole and 2'-aryl-4-Pyridyl-2,4'-bisthiazole derivatives as potential antibacterial agents0 aSynthesis and antimicrobial evaluation of novel 2aryl4aryl24Bist cFEB  a773-7870 v443 a

In continuation of our research work to explore bisthiazole derivatives as potential antimicrobial agents, herein we reported the synthesis of a series of novel 2'-aryl-4-aryl-2,4'-bisthiazole (7a-t) and 2'-aryl-4-pyridyl-2,4'-bisthiazole (9a-l) by cyclocondensation of 2-aryl thiazole-4-carbothioamide 5a-d with 2-bromo-1-arylethanone (6a-e) and bromo-1-(pyridin-2/3/4-yl)ethanone (8a-c), respectively. These novel candidates were evaluated in vitro for their antibacterial potential against four pathogenic bacteria, Escherichia coli (NCIM 2576), Pseudomonas flurescence (NCIM 2059), Staphylococcus aureus (NCIM 2602), and Bacillus subtilis (NCIM 2162). The synthesized compounds were also screened for their in vitro antifungal activity against Candida albicans (NCIM 3100). Among them, compounds 7b, 9d, 9 g, 9i, and 9 l exhibited excellent antibacterial activity with MIC 2.1 to 12.3 mu g/mL against all tested strains. Most of the compounds reported moderate antifungal activity. The pyridine ring-substituted bisthiazole reported good to excellent antibacterial activity as compared to phenyl ring-substituted bisthiazole. The potential antibacterial activity suggested that bisthiazole derivatives could assist in the development of lead compounds to treat microbial infections.

10a24'-bisthiazole10aantibacterial activity10aAntifungal activity10acyclocondensation1 aNalawade, Jitendra1 aShinde, Abhijit1 aAbhale, Yogita, K.1 aNandurkar, Yogesh1 aBobade, Vivek, D.1 aSarkar, Dhiman1 aMhaske, Pravin, C. uhttps://library.ncl.res.in/content/synthesis-and-antimicrobial-evaluation-novel-2-aryl-4-aryl-24-bisthiazole-and-2-aryl-4