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

Faculty Pharmacy Year: 2025
Type of Publication: ZU Hosted Pages:
Authors:
Journal: Scientific Reports Springer Nature Volume:
Keywords : Dual α-amylase , α-glucosidase inhibition , 1,2,4-triazole derivatives    
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 findings position triazole-based scaffolds as promising candidates for the development of next-generation antidiabetic therapies.
    
     
 
       

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