Synthesis and biological evaluation of new substituted 3-[4- (phenylsulfonamido)benzoyl]-2 H -1-benzopyran-2-one derivatives as α -glucosidase inhibitors

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 the para-position of the a-ring were synthesized and in vitro biological activities were evaluated as nonsugar α-glucosidase inhibitors. most of the test compounds demonstrated significant α-glucosidase inhibitory activity relative to that of acarbose (ic50 = 29.26 m). the para-substitution with a methoxy group or halogens could notably increase the potency. compounds 17,18,and 23,with ic50 values of 0.025 m,0.014 m,and 0.018 m,respectively,may be of significance for the further development of new nonsugar α-glucosidase inhibitors. © 2014 yu-ling wang et al.