A novel class of hydroxycoumarin derivatives were found to be potent α-glucosidase inhibitors. Their syntheses were reported and the structure− activity relationship was established. Kinetic enzymatic assays indicated that compound 10 was a slow-binding and noncompetitive inhibitor with a K i value of 589 nM, while compound 11 was a competitive inhibitor with a K i value of 4.810 μM. Among all hydroxycoumarin derivatives studied, ...