Conformationally restricted indolopiperidine derivatives as potent CCR2B receptor antagonists

被引:39
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
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.
引用
收藏
页码:2177 / 2180
页数:4
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