Conformationally restricted indolopiperidine derivatives as potent CCR2B receptor antagonists

被引：40
作者：
Witherington, J
Bordas, V
Cooper, DG
Forbes, IT
Gribble, AD
Ife, RJ
Berkhout, T
Gohil, J
Groot, PHE
机构：
[1] GlaxoSmithKline Pharmaceut, Dept Discovery Chem, Harlow CM19 5AD, Essex, England
[2] GlaxoSmithKline Pharmaceut, Dept Vasc Biol, Harlow CM19 5AD, Essex, England
来源：
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2001年 / 11卷 / 16期
关键词：
D O I：
10.1016/S0960-894X(01)00397-3
中图分类号：
R914 [药物化学];
学科分类号：
100701 ;
摘要：
The preparation and biological evaluation of a series of indolopiperidine CCR2B receptor antagonists possessing a conformationally restricted C-5 linker chain in combination with a restricted piperidine ring are described. Compared to the parent compound 1, analogue 8 shows a dramatic improvement in selectivity against a range of 5-HT and dopaminergic receptors. (C) 2001 Elsevier Science Ltd. All rights reserved.
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收藏
页码：2177 / 2180
页数：4
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