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

摘要

In the course of studies directed toward the discovery of novel non-sugar alpha-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 alpha-glucosidase inhibitors. Most compounds showed good inhibitory activity with IC(50) values ranging from 0.0645 microM to 26.746 microM. 7-Hydroxy-6-methoxy-3-[4-(4-methylphenylsulfonamido)benzoyl]-2H-1-benzopyran-2-on e 7u manifested the most potent inhibitory activity with an IC(50) value of 0.0645 microM.