insights about indole alkaloids from natural products and synthetic SAPK inhibitors along with their inhibitory properties against S. aureus and MRSA strains. This review also describes essential structural features and Structure-Activity Relationship (SAR) for SAPK inhibition.
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-1Hbenzo[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 μg/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.
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