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<p>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 (IC<sub>50</sub> = 0.27 ± 0.01&#xa0;µg/mL and 0.31 ± 0.01&#xa0;μg/mL, respectively), surpassing acarbose, and also demonstrated potent α-amylase inhibition (IC<sub>50</sub> = 0.19 ± 0.01&#xa0;μg/mL and 0.26 ± 0.01&#xa0;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.</p>

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

  • 期刊论文

  • 出版模式：

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  • 发表日期：

    2025年7月25日

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  • Mohammed A. Marzouk,
  • Elsayed M. Mahmoud,
  • Wesam S. Shehab,
  • Sherif M. Fawzy,
  • Samar M. Mohammed,
  • Mahmoud Ashraf Abdel-Razek,
  • Ghada E. Khedr,
  • Doaa A. Elsayed

摘要

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.