Partial structures of ketoconazole as modulators of the large conductance calcium-activated potassium channel (BKCa)

被引：11

作者：

Power, EC

Ganellin, CR

Benton, DCH

机构：

[1] UCL, Dept Chem, London WC1H 0AJ, England

[2] UCL, Dept Pharmacol, London WC1E 6BT, England

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2006年 / 16卷 / 04期

关键词：

potassium channels; opener; blocker; large conductance; BK(Ca);

D O I：

10.1016/j.bmcl.2005.11.001

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

A series of partial structures of ketoconazole has been synthesized and tested for activity on the large conductance calcium-activated potassium channel (BK) in bovine smooth muscle cells. This has provided openers and blockers of the channel. The results suggest that the phenyl and phenoxy moieties are important for interaction with BK, whereas the imidazole group is unimportant. The properties of the phenoxy moiety seem to determine whether the compounds act to open or block. the channel. (c) 2005 Elsevier Ltd. All rights reserved.

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页码：887 / 890

页数：4

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