Design, Synthesis and Evaluation of Schiff base derivatives of Isatin as Antibacterial agents

A novel series of Schiff bases derivatives of isatin has been designed, synthesized, and evaluated for antibacterial activity against Staphylococcus aureus (S. aureus) and Escherichia coli (E. coli). The binding mode of the designed compounds was investigated in the active site of enzyme peptide deformylase of E.coli and S. aureus respectively. Eighteen compounds were designed based on a literature review and docked against peptide deformylase catalytic cavity. All new compounds were tested for in vitro antibacterial activity against a variety of Gram positive and Gram-negative bacterial strains, such as S. aureus and E. coli, using the broth dilution method standard using actinonin and quercetin as references. The compound-14 and 5 showed the highest mol dock score in the docking study as well as good in vitro antibacterial activity minimum inhibitory concentration (MIC) against S. aureus and E. coli at 50µg/ml than standard drug quercetin. The minimum inhibitory concentration (MIC) determination revealed that the molecules were more active against Gram positive bacteria than Gram negative bacteria. The compounds demonstrated promising antibacterial properties, with MICs ranging from 25 to 50µg/ml.