Quinazolinone-1,2,3-triazole-acetamide conjugates as potent α-glucosidase inhibitors: synthesis, enzyme inhibition, kinetic analysis, and molecular docking study.

ABSTRACT: In this study, new hybrids of quinazolinone-1,2,3-triazole-acetamide were designed, synthesized, and screened for their α-glucosidase inhibitory activity. The results obtained from the in vitro screening indicated that all analogs exhibited significant inhibitory activity against α-glucosidase (IC₅₀ values ranging from 4.8-140.2 μM) in comparison to acarbose (IC₅₀ = 750.0 μM). The limited structure-activity relationships suggested the variation in the inhibitory activities of the compounds affected by different substitutions on the aryl moiety. The enzyme kinetic studies of the most potent compound 9c, revealed that it inhibited α-glucosidase in a competitive mode with a K _i value of 4.8 μM. In addition, molecular docking studies investigated

SUBMITTER: Moghadam Farid S 

PROVIDER: S-EPMC10033893 | biostudies-literature | 2023 Mar

REPOSITORIES: biostudies-literature