In the course of studies directed toward the discovery of novel non-sugar α-glucosidase inhibitors for the treatment of diabetes, a series of 3-[4-(phenylsulfonamido) benzoyl]-2H-1- benzopyran-2-one derivatives was synthesized and evaluated as α-glucosidase inhibitors. Most compounds showed good inhibitory activity with IC50 values ranging from 0.0645 μM to 26.746 μM. 7-Hydroxy-6-methoxy-3-[4-(4-methylphenylsulfonamido) benzoyl]-2H-1- ...