Synthesis and biological evaluation of a novel series of 1,5-benzothiazepine derivatives as potential antimicrobial agents

Two series of novel 1,5-benzothiazepine derivatives (23 compounds) were efficiently synthesized and evaluated for antibacterial and antifungal activities. The results indicated that the compounds possessed a broad spectrum of activity against the tested microorganisms and showed higher activity against fungi than bacteria. Compound 2e exhibited the greatest antimicrobial activity. Preliminary study of the structure–activity relationship revealed that substituents in phenyl rings had a great effect on the antimicrobial activity of these compounds.

Graphical abstractSynthesis and biological evaluation of novel 1,5-benzothiazepine derivatives are reported in this paper. Figure optionsDownload full-size imageDownload as PowerPoint slide