Synthesis and antimycobacterial screening of new thiazolyl-oxazole derivatives

TitleSynthesis and antimycobacterial screening of new thiazolyl-oxazole derivatives
Publication TypeJournal Article
Year of Publication2017
AuthorsAbhale, YK, Sasane, AV, Chavan, AP, Shekh, SHusen, Deshmukh, KK, Bhansali, S, Nawale, L, Sarkar, D, Mhaske, PC
JournalEuropean Journal of Medicinal Chemistry
Date PublishedMAY
Type of ArticleArticle

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.

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Organic Chemistry