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the MRI screening protocol.Aim Keeping in view the side effects associated with clinically used α-glucosidase inhibitors, novel thiazolidinedione-isatin hybrids were synthesized and evaluated by in vitro, in vivo and in silico procedures. Materials methods Biological evaluation, cytotoxicity assessment, molecular docking, binding free energy calculations and molecular dynamics studies were performed for hybrids. Results The most potent inhibitor A-10 (IC50 = 24.73 ± 0.93 μM) was competitive in manner and observed as non-cytotoxic.