Design and Synthesis of Novel Isoquinoline-3-nitriles as Orally Bioavailable Kv1.5 Antagonists for the Treatment of Atrial Fibrillation
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- 作者：B. Wesley Trotter ; Kausik K. Nanda ; Nathan R. Kett ; Christopher P. Regan ; Joseph J. Lynch ; Gary L. Stump ; Laszlo Kiss ; Jixin Wang ; Robert H. Spencer ; Stefanie A. Kane ; Rebecca B. White ; Rena Zhang ; Ke
- 刊名：Journal of Medicinal Chemistry
- 出版年：2006
- 出版时间：November 30, 2006
- 年：2006
- 卷：49
- 期：24
- 页码：6954 - 6957
- 全文大小：213K
- 年卷期：v.49,no.24(November 30, 2006)
- ISSN：1520-4804
文摘
Novel 3-cyanoisoquinoline Kv1.5 antagonists have beenprepared and evaluated in in vitro and in vivo assays for inhibition ofthe Kv1.5 potassium channel and its associated cardiac potassiumcurrent, IKur. Structural modifications of isoquinolinone lead 1 affordedcompounds with excellent potency, selectivity, and oral bioavailability.