Synthesis, in vitro and in vivo evaluation of 2-aryl-4H-chromene and 3-aryl-1H-benzo[f]chromene derivatives as novel α-glucosidase inhibitors.

•Series of novel 2-aryl-4H-chromene and 3-aryl-1H-benzo[f]chromenes were synthesized.•Four compounds were identified as potent α-glucosidase inhibitors.•Structure-activity relationships were derived via molecular modeling.•Lead compound 6a is superior to acarbose with IC50 of 62.26 µM.•Lead compound 6a effectively prevents postprandial hyperglycemia in rats.