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

本研究考慮到含有吲哚和羧酰胺-1,2,3-三唑-N-苯基乙酰胺分子的強(qiáng)效α-葡萄糖苷酶抑制劑，設(shè)計(jì)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。這些化合物是通過點(diǎn)擊反應(yīng)合成的，并針對(duì)酵母α-葡萄糖苷酶進(jìn)行了評(píng)估。與作為標(biāo)準(zhǔn)抑制劑的阿卡波糖相比，所有新標(biāo)題化合物都表現(xiàn)出更高的效力。特別是化合物 5k 對(duì)α-葡萄糖苷酶的抑制活性最佳，與標(biāo)準(zhǔn)抑制劑相比，抑制效果提高了約 28 倍。該化合物在動(dòng)力學(xué)上表現(xiàn)出競爭性抑制。分子對(duì)接和動(dòng)力學(xué)研究表明，化合物 5k 具有良好的結(jié)合能，能很好地占據(jù)α-葡萄糖苷酶的活性位點(diǎn)。

本文章由計(jì)算機(jī)程序翻譯，如有差異，請以英文原文為準(zhǔn)。

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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