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

Eur J Med Chem. 2009 Jul;44(7):2815-21. doi: 10.1016/j.ejmech.2008.12.021. Epub 2008 Dec 25.


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.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Anti-Infective Agents / chemical synthesis*
  • Anti-Infective Agents / chemistry
  • Anti-Infective Agents / pharmacology*
  • Bacteria / drug effects
  • Candida albicans / drug effects
  • Drug Design*
  • Structure-Activity Relationship
  • Thiazepines / chemical synthesis*
  • Thiazepines / chemistry
  • Thiazepines / pharmacology*


  • 1,5-benzothiazepine
  • Anti-Infective Agents
  • Thiazepines