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.Synthesis and biological evaluation of novel 1,5-benzothiazepine derivatives are reported in this paper.

A series of novel 1,5-benzothiazepine derivatives containing COOC2H5/COONa groups at the C(2)-position were synthesized and evaluated for their antifungal and antibacterial activities by both disc diffusion and minimal inhibition concentration (MIC) methods. Most of the compounds have been shown to have moderate to good antibacterial activity against S. aureus, S. epidermidis and excellent antifungal activity against C. albicans.