Synthesis and kinetics studies of N '-(2-(3,5-disubstituted-4H-1,2,4-triazol-4-yl)acetyl)-6/7/8-substituted-2-oxo-2H-chromen-3-carbohydrazide derivatives as potent antidiabetic agents

Abstract

A novel series of N '-(2-(3,5-disubstituted-4H-1,2,4-triazol-4-yl)acetyl)-6/7/8-substituted-2-oxo-2H-chromen-3-carbohydrazides were synthesized and studied for their alpha-glucosidase inhibition activity. Most of the synthesized compounds exhibited potential alpha-glucosidase inhibition activity with IC50 values ranging from 0.96 +/- 0.02 to 32.86 +/- 0.73 mu g/ml. Among them, compounds 3e and 4e, having a methoxy group on the coumarin ring, proved to be the most potent ones, showing an enzyme inhibition activity with IC50 = 0.96 +/- 0.02 and 1.44 +/- 0.06 mu g/ml, respectively. the kinetic study through Lineweaver-Burk plots revealed that the inhibition mechanism of the most active compounds 3d, 3e, 4d, and 4e, on the alpha-glucosidase activity, was found to be in the competitive mode.