Synthesis and biological evaluation of 1,4-diazepane derivatives as T-type calcium channel blockers

被引：19
作者：
Gu, Su Jin [1 ,2 ]
Lee, Jae Kyun [1 ]
Pae, Ae Nim [1 ]
Chung, Hye Jin [1 ]
Rhim, Hyewon [1 ]
Han, So Yeob [2 ]
Min, Sun-Joon [1 ]
Cho, Yong Seo [1 ]
机构：
[1] Korea Inst Sci & Technol, Life Hlth Div, Seoul 130650, South Korea
[2] Ewha Womans Univ, Dept Chem & Nano Sci, Seoul 130701, South Korea
来源：
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2010年 / 20卷 / 09期
关键词：
T-type calcium channel blockers; 1,4-Diazepane; Pharmacokinetics; CA2+ CHANNELS; DESIGN; ANTAGONISTS; MIBEFRADIL; DISCOVERY;
D O I：
10.1016/j.bmcl.2010.03.084
中图分类号：
R914 [药物化学];
学科分类号：
100701 ;
摘要：
We have synthesized and biologically evaluated 1,4-diazepane derivatives as T-type calcium channel blockers. In this study, we discovered compound 4s, a potential T-type calcium channel blocker with good selectivity over hERG and N-type calcium channels. In addition, it exhibited favorable pharmacokinetic characteristics for further investigation of T-type calcium channel related diseases. (C) 2010 Elsevier Ltd. All rights reserved.
引用
收藏
页码：2705 / 2708
页数：4
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