New Biscoumarin Derivatives as Potent α-Glucosidase Inhibitors: Synthesis, Biological Evaluation, Kinetic Analysis, and Docking Study

A new series of biscoumarin derivatives3a-nwere synthesized and evaluated for their alpha-glucosidase inhibitory activities. The reaction of the 4-aminocoumarin with benzaldehyde derivatives led to the formation of the title compounds in good yields. All the synthesized compounds showed potent alpha-glucosidase inhibitory activity with IC(50)ranging from 20.0 +/- 0.7 to180.1 +/- 0.8 mu M, in comparison with acarbose as the standard drug (IC50= 750.0 1.5 mu M). Among the synthesized compounds, 3,3'-(p-tolylmethylene)bis(4-amino-2H-chromen-2-one)3cwas found to be the most active compound with an IC(50)value of 20.0 +/- 0.7 mu M. Kinetic study exhibited that compound3cwas a competitive inhibitor against alpha-glucosidase (K-i= 22.4 mu M). In silico docking study for the most potent compound3cwas also performed.