Benzoylquinazolinone derivatives as new potential antidiabetic agents: α‐Glucosidase inhibition, kinetic, and docking studies,Journal of the Chinese Chemical Society

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Benzoylquinazolinone derivatives as new potential antidiabetic agents: α‐Glucosidase inhibition, kinetic, and docking studies
Journal of the Chinese Chemical Society ( IF 1.6 ) Pub Date : 2019-11-24 , DOI: 10.1002/jccs.201900268
Maryam Mohammadi‐Khanaposhtani ₁ , Hoda Yahyavi ₂ , Somaye Imanparast ₃ , Fereshte Nazemi Harandi ₄ , Mohammad Ali Faramarzi ₃ , Alireza Foroumadi ₂ , Bagher Larijani ₅ , Mahmood Biglar ₅ , Mohammad Mahdavi ₅

Affiliation

Benzoylquinazolinone derivatives 3a–n were synthesized via a simple one‐step reaction, and evaluated for in vitro α‐glucosidase inhibitory activity. Compounds 3d, 3f–g, 3i, and 3m–n showed more inhibitory activity than standard drug acarbose (IC₅₀ = 750.0 ± 1.5 μM), and among them, compound 3d displayed the highest α‐glucosidase inhibitory activity (IC₅₀ = 261.6 ± 0.1 μM). The kinetic analysis of the compound 3d revealed that this compound inhibited α‐glucosidase in a competitive manner (K_i = 255 μM). The docking studies were applied to predict binding modes of the synthesized compounds in active site of α‐glucosidase.

中文翻译：

苯甲酰喹唑啉酮衍生物作为新的潜在抗糖尿病药：α-葡萄糖苷酶抑制，动力学和对接研究

苯甲酰基喹唑啉酮衍生物3a–n通过简单的一步反应合成，并评估了其体外α-葡萄糖苷酶抑制活性。化合物3d，3f–g，3i和3m–n表现出比标准阿卡波糖更高的抑制活性（IC ₅₀ = 750.0±1.5μM），其中，化合物3d表现出最高的α-葡萄糖苷酶抑制活性（IC ₅₀ = 261.6） ±0.1μM）。化合物3d的动力学分析表明，该化合物以竞争性方式抑制了α-葡萄糖苷酶（K _i= 255μM）。对接研究用于预测合成的化合物在α-葡萄糖苷酶活性位点的结合模式。

更新日期：2019-11-24

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