Linked pyridinyl-thiadiazoles: Design and synthesis as potential candidate for treatment of XDR and MDR tuberculosis

• 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.

A 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 as PowerPoint slide