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
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
收藏
页码:5089 / 5093
页数:5
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