Abstract
The current studies mainly demonstrate the coumarin based azomethine-clubbed thiazoles synthesis and their invitro evaluation for the first time against alpha-glucosidase. Due to the catalytic role of alpha-glucosidase, it has become a precise target for the treatment of type diabetes mellitus (T2DM). The high rate of prevalence of diabetes and its associated health related problems led us to scrutinize the anti-diabetic capability of the synthesized thiazole derivatives (6a-6k). The anticipated structures of prepared compounds were confirmed through FT-IR and NMR spectroscopic methods. All the compounds showed several times potent activity than the standard drug, acarbose (IC50 = 873.34 +/- 1.67 mu M) against alpha-glucosidase with IC50 values in range of 0.87 +/- 0.02-322.61 +/- 1.14 mu M. The compound 6k displayed the highest anti-diabetic activity (IC50 = 1.88 +/- 0.03 mu M). Kinetic study revealed that these are competitive inhibitors for alpha-glucosidase. The mode of binding of the synthesized molecules were further evaluated by molecular docking, which reflects the importance of azomethine group in protein-ligand interaction. The docking scores are complementary with the IC50 values of compounds while the interaction pattern of the compounds clearly demonstrates their structure-activity relationship. Current study reported medicinal importance of thiazole derivative as future drug candidates for the management of Type 2 Diabetes Mellitus (T2DM).