期刊
JOURNAL OF MEDICINAL CHEMISTRY
卷 53, 期 23, 页码 8252-8259出版社
AMER CHEMICAL SOC
DOI: 10.1021/jm100757r
关键词
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资金
- Marie Curie Fellowship [PIIF-GA-2008-221486]
- Hong Kong Polytechnic University
A novel class of hydroxycoumarin derivatives were found to be potent alpha-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 mu M. Among all hydroxycoumarin derivatives studied, compounds 10 and 11 exhibited the highest activities, were specific inhibitors of alpha-glucosidase, and could be exploited as the lead compounds for the development of potent alpha-glucosidase inhibitors. Compounds 10 and 11 were also selected for further discussion for the mechanism of enzymatic inhibition.
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