Synthesis and Antibacterial Evaluation of 3,4-Dihydro-1H-benzo[b]azepine-2,5-dione Derivatives

Fused-azepinones are interesting heterocyclic scaffolds present in various natural products and synthetic derivatives with potent kinase inhibition, anti-cancer, anti-inflammatory, anti-HIV, neuroprotective, anti-fouling and other biological activities. These fused-azepinones are also known for their antimicrobial activity against the Plasmodium falciparum, Leishmania, Escherichia coli, and Streptococcus pneumonia. In the present work, we synthesized a library of 3,4-dihydro-1H-benzo[b]azepine-2,5-dione derivatives and evaluated them for their antibacterial potential against a panel of bacterial pathogens. The Structure-activity relationship studies revealed the essential structural features for the promising antibacterial properties against Staphylococcus aureus and Mycobacterium tuberculosis with MIC 4-64 mu g/mL. In addition, these compounds exhibited favourable selectivity index (SI >= 10) in cytotoxicity studies. With the interesting antibacterial properties exhibited and good selectivity index, these compounds have emerged as promising candidates for further development.

Automated summary

The synthesized 3,4-dihydro-1H-benzo[b]azepine-2,5-dione derivatives showed promising antibacterial properties against Staphylococcus aureus and Mycobacterium tuberculosis, making them potential candidates for further development.