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作为新型抗糖尿病药物的 N

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2025-07-10 09:39

Mohammad Hossein Sayahi, Samira Zareei, Mohammad Halimi, Majid Alikhani, Ali Moazzam, Maryam Mohammadi-Khanaposhtani, Somayeh Mojtabavi, Mohammad Ali Faramarzi, Hossein Rastegar, Parham Taslimi, Essam H Ibrahim, Hamed A Ghramh, Bagher Larijani, Mohammad Mahdavi

摘要

本研究考虑到含有吲哚和羧酰胺-1,2,3-三唑-N-苯基乙酰胺分子的强效α-葡萄糖苷酶抑制剂，设计了一系列新型 N-苯基乙酰胺-1,2,3-三唑-吲哚-2-甲酰胺衍生物 5a-n。这些化合物是通过点击反应合成的，并针对酵母α-葡萄糖苷酶进行了评估。与作为标准抑制剂的阿卡波糖相比，所有新标题化合物都表现出更高的效力。特别是化合物 5k 对α-葡萄糖苷酶的抑制活性最佳，与标准抑制剂相比，抑制效果提高了约 28 倍。该化合物在动力学上表现出竞争性抑制。分子对接和动力学研究表明，化合物 5k 具有良好的结合能，能很好地占据α-葡萄糖苷酶的活性位点。

本文章由计算机程序翻译，如有差异，请以英文原文为准。

Design, synthesis, in vitro, and in silico anti-α-glucosidase assays of N-phenylacetamide-1,2,3-triazole-indole-2-carboxamide derivatives as new anti-diabetic agents.

In this work, a novel series of N-phenylacetamide-1,2,3-triazole-indole-2-carboxamide derivatives 5a-n were designed by consideration of the potent α-glucosidase inhibitors containing indole and carboxamide-1,2,3-triazole-N-phenylacetamide moieties. These compounds were synthesized by click reaction and evaluated against yeast α-glucosidase. All the newly title compounds demonstrated superior potency when compared with acarbose as a standard inhibitor. Particularly, compound 5k possessed the best inhibitory activity against α-glucosidase with around a 28-fold improvement in the inhibition effect in comparison standard inhibitor. This compound showed a competitive type of inhibition in the kinetics. The molecular docking and dynamics demonstrated that compound 5k with a favorable binding energy well occupied the active site of α-glucosidase.

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来源期刊

Scientific Reports

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