Racemic and chiral lactams as potent, selective and functionally active CCR4 antagonists

被引：34
|
作者：
Newhouse, B
Allen, S
Fauber, B
Anderson, AS
Eary, CT
Hansen, JD
Schiro, J
Gaudino, JJ
Laird, E
Chantry, D
Eberhardt, C
Burgess, LE
机构：
[1] Array BioPharma, Boulder, CO 80301 USA
[2] Icos Corp, Bothell, WA 98021 USA
来源：
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2004年 / 14卷 / 22期
关键词：
lactams; CCR4; antagonists;
D O I：
10.1016/j.bmcl.2004.09.001
中图分类号：
R914 [药物化学];
学科分类号：
100701 ;
摘要：
A series of racemic and chiral, nonracemic lactams that display high binding affinities, functional chemotaxis antagonism, and selectivity toward CCR4 are described. Compound 41, which provides reasonably high blood levels in mice when dosed intraperitoneally, was identified as a useful pharmacological tool to explore the role of CCR4 antagonism in animal models of allergic disease. (C) 2004 Elsevier Ltd. All rights reserved.
引用
收藏
页码：5537 / 5542
页数：6
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