Design, synthesis and antibacterial activity of isatin derivatives as FtsZ inhibitors

Seven isatin derivatives have been designed, and their chemical structures were characterized by single crystal X-ray diffraction studies, H-1 NMR, MS, and elemental analysis. Structural stabilization followed by intramolecular as well as intermolecular H-bonds makes these molecules as perfect examples in molecular recognition with self-complementary donor and acceptor units within a single molecule. These compounds were evaluated for antimicrobial activities. Docking simulations have been performed to position compounds into the FtsZ active site to determine their probable binding models. All of the compounds exhibited better antibacterial activities. Interestingly, compound 5c and 5d exhibited better antibacterial activities with IC50 values of 0.03 and 0.05 mu mol/mL against Staphylococcus aureus, respectively. Compound 5g displays antibacterial activity with IC50 values of 0.672 and 0.830 mu mol/ml, against Escherichia coli and Pseudomonas aeruginosa, respectively. (C) 2016 Elsevier B.V. All rights reserved.