Preparation of ferulic acid derivatives and evaluation of their xanthine oxidase inhibition activity

被引:14
|
作者
Wang, Feng
Yang, Leixiang
Huang, Kexin
Li, Xiaokun
Hao, Xiaojiang
Stoeckigt, Joachim
Zhao, Yu
机构
[1] Zhejiang Univ, Dept Tradit Chinese Med & Nat Drug Res, Coll Pharmaceut Sci, Hangzhou 310031, Peoples R China
[2] Wenzhou Coll Med, Sch Pharm, Wenzhou 325035, Peoples R China
[3] Key Lab Chem Nat Prod Guizhou Prov, Guiyang 550022, Peoples R China
[4] Chinese Acad Sci, Guiyang 550022, Peoples R China
[5] Univ Mainz, Inst Pharm, Lehrstuhl Pharmazeut Biol, D-55099 Mainz, Germany
关键词
ferulic acid derivatives; xanthine oxidase inhibitor; gout;
D O I
10.1080/14786410601129648
中图分类号
O69 [应用化学];
学科分类号
081704 ;
摘要
Several ferulic acid ethyl esters (3a-h) were synthesized under the Knoevengel reaction condition and they were further reduced to afford the respective allylic alcohol derivatives (4a-g). Some of them were evaluated for the xanthine oxidase (XO) inhibitory activity. Among them, 3h exhibited a significant inhibitory activity with an IC50 value of 1.35x10(-5) M, while the IC50 value of allopurinol used as the positive control was 1.49x10(-5) M. The study suggested that the higher acidity of the phenolic OH group in the ferulic acid derivatives might result in improved XO inhibitory activity.
引用
收藏
页码:196 / 202
页数:7
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