Hydroxycoumarin Derivatives: Novel and Potent α-Glucosidase Inhibitors

• DOI: 10.1021/jm100757r
• Publication Date: 2010-11-05T12:04:09Z
• Authors: Qiong Shen; Jialiang Shao; Quan Peng; Wanjin Zhang; Lin Ma; Albert S. C. Chan; Lianquan Gu
• Keywords: Lead compound; 4-Hydroxycoumarin; Enzyme Inhibition

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