Article ID Journal Published Year Pages File Type
1397237 European Journal of Medicinal Chemistry 2015 6 Pages PDF
Abstract

•Tractable small molecules are synthesised with easy, inexpensive ROS.•Analoging of newer chemotype, lead to hit 7f.•Reported here antimycobacterial activity of 7f with 25 clinical isolates.•Toxicity profile of 7f is observed minimal.

Multi-drug resistant (MDR) and extremely drug resistant (XDR) Mycobacterium tuberculosis strains have turned tuberculosis (TB) as “on the verge of eradication” to “most life threatening” disease. Furthermore, synergy with HIV and other immunosuppressive disease have strengthened its prevalence. This research reports small molecule anti-infectives which are specifically potent against several strains and isolates of TB. The hit compound 7f has also proved to be active against almost 25 clinical isolates comparable to marketed anti-TB agents.

Graphical abstractA substituted pyridinyl-thiadizole has been identified and then modified to yield 7f, a potent antitubercular agent. The anti-XDR & MDR-TB activity is discussed using 25 different isolates.Figure optionsDownload full-size imageDownload as PowerPoint slide

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Physical Sciences and Engineering Chemistry Organic Chemistry
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