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...
Gespeichert in:
Veröffentlicht in: | Bioorganic & medicinal chemistry letters 2012-03, Vol.22 (5), p.1917-1921 |
---|---|
Hauptverfasser: | , , , , , |
Format: | Artikel |
Sprache: | eng |
Schlagworte: | |
Online-Zugang: | Volltext |
Tags: |
Tag hinzufügen
Keine Tags, Fügen Sie den ersten Tag hinzu!
|
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 |