Design, Synthesis, In‐Vivo Anti‐Diabetic Activity, In‐Vitro α‐Glucosidase Inhibitory Activity and Molecular Docking Studies of Some Quinazolinone Derivatives

A new series of quinazolinone bearing acetamide derivatives were designed and synthesized. The designed compounds were tested for their in vivo anti‐hyperglycemic effects against STZ‐induced hyperglycemic rats. Compound 10 a displayed the strongest hypoglycemic effect with blood glucose level reduction of 43.75 %. Besides, congeners 10 e , 10 i , 10 j , and 11 c strongly reduced the glucose level with percent reduction of 33.08, 30.00, 35.00, and 32.83 %, respectively. The most active members were then evaluated for their ability to inhibit Saccharomyces cerevisiae α‐glucosidase using BioVision α‐Glucosidase Inhibitor Screening Kit. Compounds 10 a and 11 c possessed potent α‐glucosidase inhibitory activity with IC 50 values of 649 and 715 μM, respectively. Molecular docking study against the α‐glucosidase homology model was performed to understand the molecular interactions between the molecule and enzyme.