Thiazolyl-pyrazole derivatives as potential antimycobacterial agents

TitleThiazolyl-pyrazole derivatives as potential antimycobacterial agents
Publication TypeJournal Article
Year of Publication2019
AuthorsTakate, SJ, Shinde, AD, Karale, BK, Akolkar, H, Nawale, L, Sarkar, D, Mhaske, PC
JournalBioorganic & Medicinal Chemistry Letters
Date PublishedMAY
Type of ArticleArticle
Keywordsantimycobacterial activity, Cytotoxicity, Pyrazole, thiazoles

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 > 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.

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Organic Chemistry