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

Gu, Su Jin; Lee, Jae Kyun; Pae, Ae Nim; Chung, Hye Jin; Rhim, Hyewon; Han, So Yeob; Min, Sun-Joon; Cho, Yong Seo

doi:10.1016/j.bmcl.2010.03.084

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

Gu, Su Jin;
Lee, Jae Kyun;
Pae, Ae Nim;
Chung, Hye Jin;
Rhim, Hyewon;
... Min, Sun-Joon;
외 2명

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21

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22

초록

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.

키워드

T-type calcium channel blockers; 1,4-Diazepane; Pharmacokinetics; CA2+ CHANNELS; DESIGN; ANTAGONISTS; MIBEFRADIL; DISCOVERY

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

저자: Gu, Su Jin; Lee, Jae Kyun; Pae, Ae Nim; Chung, Hye Jin; Rhim, Hyewon; Han, So Yeob; Min, Sun-Joon; Cho, Yong Seo

DOI: 10.1016/j.bmcl.2010.03.084

발행일: 2010-05

유형: Article

저널명: Bioorganic & Medicinal Chemistry Letters

권: 20

호: 9

페이지: 2705 ~ 2708

언어: ENG

출판사: PERGAMON-ELSEVIER SCIENCE LTD

발행국가: 영국

분량: 4 페이지

ISSN: E 1464-3405
P 0960-894X