Hydroxycoumarin Derivatives: Novel and Potent α-Glucosidase Inhibitors

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• 作者：Qiong Shen ; Jialiang Shao ; Quan Peng ; Wanjin Zhang ; Lin Ma ; Albert S. C. Chan ; Lianquan Gu
• 刊名：Journal of Medicinal Chemistry
• 出版年：2010
• 出版时间：December 9, 2010
• 年：2010
• 卷：53
• 期：23
• 页码：8252-8259
• 全文大小：932K
• 年卷期：v.53,no.23(December 9, 2010)
• ISSN：1520-4804

文摘

A novel class of hydroxycoumarin derivatives were found to be potent α-glucosidase inhibitors. Their syntheses were reported and the structure−activity relationship was established. Kinetic enzymatic assays indicated that compound 10 was a slow-binding and noncompetitive inhibitor with a K_i value of 589 nM, while compound 11 was a competitive inhibitor with a K_i value of 4.810 μM. Among all hydroxycoumarin derivatives studied, compounds 10 and 11 exhibited the highest activities, were specific inhibitors of α-glucosidase, and could be exploited as the lead compounds for the development of potent α-glucosidase inhibitors. Compounds 10 and 11 were also selected for further discussion for the mechanism of enzymatic inhibition.