Microwave assisted synthesis and biological evaluation of a series of 1,5-benzothiazepines as potential cytotoxic and antimicrobial agents

Abstract

A series of 2,3-dihydro-2-(susbtituted)-4-(1-methyl-1 H -pyrrol-2-yl)-1,5-benzothiazepines (4a-v) have been synthesized evaluated for their in vitro cytotoxicity and antimicrobial activities. Among the tested compounds for cytotoxicity using Brine shrimp lethality assay, compound 4q exhibited significant cytotoxicity at ED 50 values 3.45±0.15 µg/mL. This level of activity was found comparable to that of the reference drug podophyllotoxin with ED 50 value 3.61±0.17 µg/mL. Antimicrobial activity was assessed using agar well diffusion assay method against selected Gram-positive, Gram-negative and fungal strains. Among the compounds tested, 4q, 4r and 4l were found to be more active with MIC 16-32 µg/mL against all tested microorganisms.