期刊
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
卷 45, 期 11, 页码 5064-5070出版社
ELSEVIER FRANCE-EDITIONS SCIENTIFIQUES MEDICALES ELSEVIER
DOI: 10.1016/j.ejmech.2010.08.015
关键词
Urease inhibitor; Helicobacter pylori; Pyrogallol derivatives; Catechol derivatives; Autodock
资金
- Scientific Research Fund of Hunan Provincial Education Department of China [09B083]
- Key Laboratory of Hunan Forest Products and Chemical Industry Engineering of China [JDZ200904]
Some pyrogallol and catechol derivatives were synthesized, and their urease inhibitory activity was evaluated by using acetohydroxamic acid (AHA), a well known Helicobacter pylori urease inhibitor, as positive control. The assay results indicate that many compounds have showed potential inhibitory activity against H. pylori urease. 4-(4-Hydroxyphenethyl)phen-1,2-diol (2a) was found to be the most potent urease inhibitor with IC(50)s of 1.5 +/- 0.2 mu M for extracted fraction and 4.2 +/- 0.3 mu M for intact cell, at least 10 times and 20 times lower than those of AHA (IC50 of 17.2 +/- 0.9 mu M, 100.6 +/- 13 mu M), respectively. This finding indicate that 2a would be a potential urease inhibitor deserves further research. Molecular dockings of 2a into H. pylori urease active site were performed for understanding the good activity observed. (C) 2010 Elsevier Masson SAS. All rights reserved.
作者
我是这篇论文的作者
点击您的名字以认领此论文并将其添加到您的个人资料中。
推荐
暂无数据