Synthesis and antimicrobial activity of azepine and thiepine derivatives

Abstract

A series of new 5H-pyridobenzazepine and pyridobenzothiepine derivatives was synthesized by Pd-catalyzed formation of C-N and C-S bonds. All synthesized compounds were tested for their in vitro antimicrobial activity. The 5H-pyridobenzazepine derivatives showed better antibacterial and antifungal activity than corresponding 5H-dipyridoazepine analogs. Among the synthesized azepines, derivative 8 displayed potent activity against tested bacteria (MIC = 39-78 μg/mL), while azepine 12 showed promising antifungal activity (MIC = 156-313 μg/mL). The synthesized thiepine derivatives exhibited weak antibacterial activity, but showed pronounced antifungal activity. [Projekat Ministarstva nauke Republike Srbije, br. 172008]

Keywords

• azepines
• thiepines
• heterocycles
• palladium
• antibacterials
• anti-fungal