Discovery and synthesis of a novel series of quinoline-based thrombin receptor (PAR-1) antagonists

被引：18
|
作者：
Clasby, MC
Chackalamannil, S
Czarniecki, M
Doller, D
Eagen, K
Greenlee, WJ
Lin, Y
Tsai, H
Xia, Y
Ahn, HS
Agans-Fantuzzi, J
Boykow, G
Chintala, M
Foster, C
Bryant, M
Lau, J
机构：
[1] Schering Plough Corp, Res Inst, Cent Nervous Syst & Cardiovasc Chem Res, Kenilworth, NJ 07033 USA
[2] Schering Plough Corp, Res Inst, Cardiovasc & Metab Dis Res, Kenilworth, NJ 07033 USA
[3] Schering Plough Corp, Res Inst, Drug Metab & Pharmacokinet Res, Kenilworth, NJ 07033 USA
来源：
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2006年 / 16卷 / 06期
关键词：
thrombin; receptor; antagonist; PAR-1; quinoline;
D O I：
10.1016/j.bmcl.2005.12.042
中图分类号：
R914 [药物化学];
学科分类号：
100701 ;
摘要：
The design, synthesis, and SAR studies of a structurally novel series of highly potent thrombin receptor (PAR-1) antagonists are described. Compound 30 is a highly potent thrombin receptor antagonist (IC50 = 6.3 nM), a related compound 36 showing efficacy in a monkey ex vivo study. (C) 2005 Elsevier Ltd. All rights reserved.
引用
收藏
页码：1544 / 1548
页数：5
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