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

被引：53

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

页码：3379 / 3384

页数：6

共 33 条

[21] SELECTIVE-INHIBITION OF T-TYPE CA2+ CHANNELS BY RO-40-5967 [J].