Synthesis of Novel molecular hybrid 3-(4,5-dihydro-1H-pyrazol-3-yl)-4-hydroxy-2H-chromen-2-one derivatives and In Vitro α-glucosidase and α-amylase inhibitory activity

Abstract

A novel series of 3-(4,5-dihydro-1H-pyrazol-3-yl)-4-hydroxy-2H-chromen-2-one derivatives was designed based on molecular hybridization technique. A series of 3-(1-benzoyl-5-phenyl-4,5-dihydro-1H-pyrazol-3-yl)-4-hydroxy-2H-chromen-2-one derivatives (6a-6p) that incorporate a variety of substituents at the 2 and 4 position of the benzyl moiety have been synthesized. These compounds were evaluated for their antidiabetic activity against α-glucosidase and α-amylase. The biological screening indicates that these hybrid derivatives exhibited promising IC50 values in the range of 91.24μM -261.82μM and 85.03μM -237.78μM respectively. Two analogs, 6j and 6m have shown most potential activity against both α-glucosidase and α-amylase were identified as potent antidiabetic agents.