3-Thio-quinolinone maxi-K openers for the treatment of erectile dysfunction

被引：46

作者：

Boy, KM ^{[1
]}

Guernon, JM ^{[1
]}

Sit, SY ^{[1
]}

Xie, K ^{[1
]}

Hewawasam, P ^{[1
]}

Boissard, CG ^{[1
]}

Dworetzky, SI ^{[1
]}

Natale, J ^{[1
]}

Gribkoff, VK ^{[1
]}

Lodge, N ^{[1
]}

Starrett, JE ^{[1
]}

机构：

[1] Bristol Myers Squibb Co, Pharmaceut Res Inst, Wallingford, CT 06492 USA

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2004年 / 14卷 / 20期

关键词：

maxi-K; BK; potassium channels; erectile dysfunction;

D O I：

10.1016/j.bmcl.2004.07.080

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

A series of Maxi-K openers for the treatment of erectile dysfunction based on the 3-thio-quinolinone core is described. Significant levels of channel opening (up to 550% of control) are seen in transfected oocytes. Functional activity in rabbit corpus cavernosum tissue strips confirms the potential to effect therapy for ED, the effect being maximal for the 3-amino-2-hydroxy thiol side chain. (C) 2004 Elsevier Ltd. All rights reserved.

引用

页码：5089 / 5093

页数：5

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