Novel 5-cyclopropyl-1,4-benzodiazepin-2-ones as potent and selective IKs-blocking Class III antiarrhythmic agents

被引:15
作者
Butcher, JW [1 ]
Liverton, NJ
Claremon, DA
Freidinger, RM
Jurkiewicz, NK
Lynch, JJ
Salata, JJ
Wang, JX
Dieckhaus, CM
Slaughter, DE
Vyas, K
机构
[1] Merck Res Labs, Dept Med Chem, W Point, PA 19486 USA
[2] Merck Res Labs, Dept Pharmacol, W Point, PA 19486 USA
[3] Merck Res Labs, Dept Drug Metab, W Point, PA 19486 USA
关键词
D O I
10.1016/S0960-894X(03)00049-0
中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
Novel 5-cyclopropyl-1,4-benzodiazepin-2-ones having various N-1 substituents were identified as potent and selective blockers of the slowly activating cardiac delayed rectifier potassium current (I-Ks). Compound 11 is the most potent I-Ks channel blocker reported to date. (C) 2003 Elsevier Science Ltd. All rights reserved.
引用
收藏
页码:1165 / 1168
页数:4
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