Inhibition of jack bean urease by organobismuth compounds

被引:24
作者
Murafuji, T [1 ]
Azuma, T
Miyoshi, Y
Ishibashi, M
Rahman, AFMM
Migita, K
Sugihara, Y
Mikata, Y
机构
[1] Yamaguchi Univ, Fac Sci, Dept Chem, Yamaguchi 7538512, Japan
[2] Nara Womens Univ, Fac Sci, Dept Chem, Nara 6308506, Japan
基金
日本学术振兴会;
关键词
bismuth; organobismuth; jack bean urease; urease inhibitor; Helicobacter pylori;
D O I
10.1016/j.bmcl.2005.12.034
中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
Inhibitory activity of organobismuth compounds, triarylbismuthanes 1 and their dihalides 2 and 3, was examined against jack bean urease. Besides triarylbismuth dichlorides 2, triarylbismuth difluorides 3 and bismuthanes 1 exhibited the activity. Of all these compounds, triphenylbismuth difluoride 3a and tris(4-fluorophenyl)bismuth dichloride 2b showed the highest activity. These results indicate that generation of the inhibitory effect is not always governed by the Lewis acidity at the bismuth center. Such a tendency of inhibition by the organobismuth compounds is in good accord with that observed in the antibacterial activity against Helicobacter pylori, suggesting that H. pylori-produced urease may be a therapeutic target by bismuth-based drugs. (C) 2005 Elsevier Ltd. All rights reserved.
引用
收藏
页码:1510 / 1513
页数:4
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