Synthesis and Biological Evaluation of 3-Styrylchromone Derivatives as Free Radical Scavengers and α-Glucosidase Inhibitors

被引:24
|
作者
Takao, Koichi [1 ]
Ishikawa, Ryo [1 ]
Sugita, Yoshiaki [1 ]
机构
[1] Josai Univ, Fac Pharmaceut Sci, Dept Pharmaceut & Hlth Sci, Bioorgan Chem Lab, Sakado, Saitama 3500295, Japan
关键词
3-styrylchromone; alpha-glucosidase inhibitor; antioxidant; structure-activity relationship; 2-STYRYLCHROMONES; AGENTS; OXYGEN;
D O I
10.1248/cpb.c14-00351
中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
A series of 3-styrylchromone derivatives (4-20) were synthesized and the structure-activity relationships for alpha-glucosidase inhibition and antioxidant activities were analyzed. Among the synthesized compounds, compounds 15 and 20, which contain a catechol moiety, showed both potent 1,1-dipheny1-2-picrylhydrazyl (DPPH) free radical scavenging activity (15: EC50=17 mu m; 20: EC50=23 mu m) and alpha-glucosidase inhibitory activity (15: IC50=16 mu m; 20: IC50=10 mu m). Our data suggest that 3-styrylchromone derivatives are novel alpha-glucosidase inhibitors that have the potential to counteract diet-induced hyperglycemia in diabetes.
引用
收藏
页码:810 / 815
页数:6
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