Synthesis and evaluation of the α-glucosidase inhibitory activity of 3-[4-(phenylsulfonamido)benzoyl]-2H-1-benzopyran-2-one derivatives

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-benzopyran-2-one 7u manifested the most potent inhibitory activity with an IC50 value of 0.0645 μM.

Graphical abstractA series of 3-[4-(phenylsulfonamido)benzoyl]-2H-1-benzopyran-2-one derivatives was synthesized and evaluated as α-glucosidase inhibitors. Compound 7u showed the strongest inhibitory activity.Figure optionsDownload full-size imageDownload as PowerPoint slide