Synthesis and biological evaluation of coumarin derivatives as α-glucosidase inhibitors.,European Journal of Medicinal Chemistry

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Synthesis and biological evaluation of coumarin derivatives as α-glucosidase inhibitors.
European Journal of Medicinal Chemistry ( IF 6.0 ) Pub Date : 2019-12-30 , DOI: 10.1016/j.ejmech.2019.112013
Xue-Tao Xu ₁ , Xu-Yang Deng ₁ , Jie Chen ₁ , Qi-Ming Liang ₁ , Kun Zhang ₁ , Dong-Li Li ₁ , Pan-Pan Wu ₁ , Xi Zheng ₂ , Ren-Ping Zhou ₂ , Zheng-Yun Jiang ₂ , Ai-Jun Ma ₁ , Wen-Hua Chen ₁ , Shao-Hua Wang ₃

Affiliation

In this study, two series of coumarin derivatives 5a∼i and 6a∼i were synthesized, and their inhibitory activity against α-glucosidase was determined. The results indicated that most of the synthesized derivatives exhibited prominent inhibitory activities against α-glucosidase. Among them, compounds 5a and 5b showed the strongest inhibition with the IC50 values of 19.64 μM and 12.98 μM, respectively. Enzyme kinetic studies of compounds 5a and 5b proved that their inhibition was reversible and a mixed type. The KI and KIS values of compound 5a were calculated to be 27.39 μM and 13.02 μM, respectively, and the corresponding values for compound 5b being 27.02 μM and 13.65 μM, respectively. The docking studies showed that compound 5b could be inserted into the active pocket of α-glucosidase and form hydrogen bonds with LYS293 to enhance the binding affinity.

中文翻译：

香豆素衍生物作为α-葡萄糖苷酶抑制剂的合成及生物学评价。

在这项研究中，合成了两个系列的香豆素衍生物5a-i和6a-i，并确定了它们对α-葡萄糖苷酶的抑制活性。结果表明，大多数合成的衍生物对α-葡萄糖苷酶表现出显着的抑制活性。其中，化合物5a和5b表现出最强的抑制作用，IC50值分别为19.64μM和12.98μM。化合物5a和5b的酶动力学研究证明，它们的抑制作用是可逆的，是混合型。化合物5a的KI和KIS值分别计算为27.39μM和13.02μM，化合物5b的相应值分别为27.02μM和13.65μM。

更新日期：2019-12-30

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