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

Herein we report a study of novel arylchromene derivatives as analogs of naturally occurring flavonoids with prominent alpha-glucosidase inhibitory properties. Novel inhibitors were identified via simple stepwise in silico screening, efficient synthesis, and biological evaluation. It is shown that 2-aryl-4H-chromene core retains pharmacophore properties while being readily available synthetically. A lead compound identified through screening inhibits yeast alpha-glucosidase with IC50 of 62.26 mu M and prevents postprandial hyperglycemia in rats at 2.2 mg/kg dose.