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

被引：20

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

页码：2705 / 2708

页数：4

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