부산대학교 도서관

Graphical abstract A novel series of quinazolinone-1,2,3-triazole hybrids 10a-p were designed, synthesized, and evaluated for their in vitro α-glucosidase inhibitory activity and all them exhibited α-glucosidase inhibitory activity more than standard drug acarbose. Highlights • A novel series of quinazolinone-1,2,3-triazole hybrids 10a-p were synthesized as α-glucosidase inhibitors. • All compounds showed anti-α-glucosidase activity superior to acarbose. • Compound 10g was the most active compound that was around 6-fold more potent than acarbose. • Compound 10g was a competitive inhibitor for α-glucosidase with K i value 117 µM. • Molecular docking study confirmed the results obtained through in vitro experiments. Abstract A novel series of quinazolinone-1,2,3-triazole hybrids 10a-p were designed, synthesized, and evaluated for their in vitro α -glucosidase inhibitory activity leading to efficient anti-diabetic agents. All synthesized compounds exhibited good inhibitory activity against yeast α -glucosidase (IC 50 values in the range of 181.0–474.5 µM) even much more potent than standard drug acarbose (IC 50 = 750.0). Among them, quinazolinone-1,2,3-triazoles possessing 4-bromobenzyl moiety connected to 1,2,3-triazole ring (10g and 10p) demonstrated the most potent inhibitory activity towards α -glucosidase. Compound 10g inhibited α -glucosidase in a competitive manner with K i value of 117 µM. Furthermore, the binding modes of the most potent compounds 10g and 10p in the α -glucosidase active site was studied through in silico docking studies. Also, lack of cytotoxicity of compounds 10g and 10p was confirmed via MTT assay. [ABSTRACT FROM AUTHOR]