Synthesis and Biological Evaluation of New Substituted 3-[4-(Phenylsulfonamido)benzoyl]-2H-1-benzopyran-2-one Derivatives asα-Glucosidase Inhibitors

Abstract

A series of new substituted 3-[4-(phenylsulfonamido)benzoyl]-2H-1-benzopyran-2-one derivatives bearing groups methoxy,tert-butyl, and atoms of halogens at thepara-position of the A-ring were synthesized andin vitrobiological activities were evaluated as nonsugarα-glucosidase inhibitors. Most of the test compounds demonstrated significantα-glucosidase inhibitory activity relative to that of Acarbose (IC50= 29.26 μM). Thepara-substitution with a methoxy group or halogens could notably increase the potency. Compounds17,18, and23, with IC50values of 0.025 μM, 0.014 μM, and 0.018 μM, respectively, may be of significance for the further development of new nonsugarα-glucosidase inhibitors.