Bioorganic and Medicinal Chemistry Letters p. 1917 - 1921 (2012)
Update date:2022-09-26
Topics:
Alegaon, Shankar G.
Alagawadi, Kallanagouda R.
Sonkusare, Pranali V.
Chaudhary, Sagar M.
Dadwe, Dilip H.
Shah, Amol S.
The increase in the prevalence of multi drug-resistant and extensively drug-resistant strains of Mycobacterium tuberculosis case demonstrates the urgent need of discovering new promising compounds with antimycobacterial activity. As part of our research program and with a aim of identifying new antitubercular drug candidates, a new class of 2-(trifluoromethyl)-6- arylimidazo[2,1-b][1,3,4]thiadiazole derivatives has been synthesized by both conventional as well as microwave assisted method and evaluated for their in vitro antitubercular activity against M. tuberculosis H37Rv. Moreover, various drug-likeness properties of new compounds were predicted. Seven compounds from the series exhibited good activity with MIC in range 3.12-1.56 μg/ml. The present study suggests that compounds 6b, 6c, 6d, 6e and 6f may serve as promising lead scaffolds for further generation of new anti-TB agents.
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Doi:10.1021/ol5002126
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