Initial SAR studies on apamin-displacing 2-aminothiazole blockers of calcium-activated small conductance potassium channels

被引：39

作者：

Gentles, Robert G. ^{[1
]}

Grant-Young, Katherine ^{[1
]}

Hu, Shuanghua ^{[1
]}

Huang, Yazhong ^{[1
]}

Poss, Michael A. ^{[1
]}

Andres, Charles ^{[1
]}

Fiedler, Tracey ^{[1
]}

Knox, Ronald ^{[1
]}

Lodge, Nicholas ^{[1
]}

Weaver, C. David ^{[1
]}

Harden, David G. ^{[1
]}

机构：

[1] Bristol Myers Squibb Co, Res & Dev, Wallingford, CT 06492 USA

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2008年 / 18卷 / 19期

关键词：

2-aminothiazole; small conductance potassium channel; potassium channel blockers; apamin;

D O I：

10.1016/j.bmcl.2008.08.023

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

An initial SAR study on a series of apamin-displacing 2-aminothiazole K(Ca)2 channel blockers is described. Potent inhibitors such as N-(4-methylpyridin-2-yl)-4-(pyridin-2-yl) thiazol-2-amine (13) are disclosed, and for select members of the series, the relationship between the observed activity in a thallium flux, a binding and a whole-cell electrophysiology assay is presented. (c) 2008 Elsevier Ltd. All rights reserved.

引用

页码：5316 / 5319

页数：4

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