3,4-dihydroquinazoline derivatives as novel selective T-type Ca2+ channel blockers

被引：52
作者：
Lee, YS
Lee, BH
Park, SJ
Kang, SB
Rhim, H
Park, JY
Lee, JH
Jeong, SW
Lee, JY
机构：
[1] Kyung Hee Univ, Coll Sci, Res Inst Basic Sci, Seoul 130701, South Korea
[2] Kyung Hee Univ, Coll Sci, Dept Chem, Seoul 130701, South Korea
[3] Korea Inst Sci & Technol, Div Life Sci, Seoul 130650, South Korea
[4] Korea Univ, Dept Chem, Seoul 136701, South Korea
[5] Sogang Univ, Dept Life Sci, Seoul 121742, South Korea
[6] Yonsei Univ, Wonju Coll Med, Dept Physiol, Wonju 220701, Kangwon Do, South Korea
[7] Yonsei Univ, Wonju Coll Med, Inst Basic Med Sci, Wonju 220701, Kangwon Do, South Korea
来源：
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2004年 / 14卷 / 13期
关键词：
3,4-dihydroquinazolines; T-type calcium channel; blockers; mibefradil;
D O I：
10.1016/j.bmcl.2004.04.090
中图分类号：
R914 [药物化学];
学科分类号：
100701 ;
摘要：
For LVA T-type Ca2+ channel blockers, 3,4-dihydroquinazoline derivatives as new scaffolds were prepared and evaluated for the inhibitory activity against two members of the recombinant T-type Ca2+ channel family. Among them, 8a (KYS05001, IC50 = 0-9 muM) was nearly equipotent with mibefradil (IC50 = 0.84 muM) and inhibited LVA T-type Ca2+ channel with greater efficacy than HVA Ca2+ channel. (C) 2004 Elsevier Ltd. All rights reserved.
引用
收藏
页码：3379 / 3384
页数：6
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