Medicinal Chemistry

Design, Synthesis and Antimycobacterial Activity of Dispiropyrrolidines Derivatives

Abstract

Mohd Zaheen Hassan, Mohamed Ashraf Ali, Hasnah Osman, Raju Suresh Kumar and Natarajan Arumugam

In vitro anti-mycobacterial activities of dispiropyrrolidine derivatives along with their intermediates bisarylidene piperidones were investigated through high throughput screen. Our results revealed that dispiropyrrolidines possess promising activity against Mtb H37Rv. Compound 4g, 1-Methyl-4-(2,4-dichlorophenyl)pyrrolo-(spiro[2.3″]oxindole)- spiro[3.3′]-5′-(2,4-dichlorophenylmethylidene)piperidin-4′-one emerged as the most active antimycobacterial agent having EC50 of 2.46 μM and MIC at 10 μM against MTB-H37Rv.