Synthesis and biological evaluation of novel T-type Ca2+ channel blockers

被引：38
|
作者：
Jung, HK
Doddareddy, MR
Cha, JH
Rhim, H
Cho, YS
Koh, HY
Jung, BY
Pae, AN
机构：
[1] Korea Inst Sci & Technol, Lifesci Div, Seoul 130650, South Korea
[2] Korea Univ, Dept Chem, Seoul 136701, South Korea
来源：
BIOORGANIC & MEDICINAL CHEMISTRY | 2004年 / 12卷 / 15期
关键词：
T-type calcium channel; synthesis;
D O I：
10.1016/j.bmc.2004.06.011
中图分类号：
Q5 [生物化学]; Q7 [分子生物学];
学科分类号：
071010 ; 081704 ;
摘要：
A small molecule library of piperazinylalkylisoxazole derivatives containing about 600 compounds was designed, synthesized and evaluated for blocking effects on T-type Ca2+ channel. Several ligands were identified to possess high inhibitory activity against the T-type Ca2+ channel. The compound 21 with trifluoromethyl substituents at C-3-position of phenyl group (W) and C-2-position of phenyl group (R-2) showed the highest inhibitory activity with IC50 value of 1.02 muM, which is comparable to that of mibefradil. (C) 2004 Elsevier Ltd. All rights reserved.
引用
收藏
页码：3965 / 3970
页数：6
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