Dual α-amylase and α-glucosidase inhibition by 1,2,4-triazole derivatives for diabetes treatment.

ABSTRACT: The development of effective antidiabetic agents remains a critical challenge in diabetes management. In this study, we introduce novel 1,2,4-triazole-based derivatives designed as dual inhibitors of α-amylase and α-glucosidase, key enzymes in carbohydrate metabolism. Molecular docking identified six promising candidates, with compounds 4 and 10 showing the highest potency. Both compounds exhibited strong α-glucosidase inhibition (IC₅₀ = 0.27 ± 0.01 µg/mL and 0.31 ± 0.01 μg/mL, respectively), surpassing acarbose, and also demonstrated potent α-amylase inhibition (IC₅₀ = 0.19 ± 0.01 μg/mL and 0.26 ± 0.01 μg/mL, respectively). Structure-activity relationship analysis highlighted the crucial role of acetyl and bromo substituents in enhancing enzyme inhibition. These find

SUBMITTER: Marzouk MA 

PROVIDER: S-EPMC12297423 | biostudies-literature | 2025 Jul

REPOSITORIES: biostudies-literature