Novel imidazo[2,1-b][1,3,4]thiadiazole carrying rhodanine-3-acetic acid as potential antitubercular agents

Microwave-assisted synthesis and investigation of antitubercular profile of new 2-(trifluoromethyl)-6-arylimidazo[2,1-b][1,3,4]-thiadiazole derivatives are described. The increase in the prevalence of multi drug-resistant and extensively drug-resistant strains of Mycobacteriumtuberculosis case demon...

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Veröffentlicht in:Bioorganic & medicinal chemistry letters 2012-03, Vol.22 (5), p.1917-1921
Hauptverfasser: Alegaon, Shankar G., Alagawadi, Kallanagouda R., Sonkusare, Pranali V., Chaudhary, Sagar M., Dadwe, Dilip H., Shah, Amol S.
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Sprache:eng
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Zusammenfassung:Microwave-assisted synthesis and investigation of antitubercular profile of new 2-(trifluoromethyl)-6-arylimidazo[2,1-b][1,3,4]-thiadiazole derivatives are described. The increase in the prevalence of multi drug-resistant and extensively drug-resistant strains of Mycobacteriumtuberculosis 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 3.12–1.56μg/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.
ISSN:0960-894X
1464-3405
DOI:10.1016/j.bmcl.2012.01.052