2-Amino-5-aryl-pyridines as selective CB2 agonists: Synthesis and investigation of structure-activity relationships

被引:11
|
作者
Gleave, Robert J. [1 ]
Beswick, Paul J. [1 ]
Brown, Andrew J. [1 ]
Giblin, Gerard M. P. [1 ]
Haslam, Carl P. [1 ]
Livermore, David [1 ]
Moses, Andrew [1 ]
Nicholson, Neville H. [1 ]
Page, Lee W. [1 ]
Slingsby, Brian [1 ]
Swarbrick, Martin E. [1 ]
机构
[1] GlaxoSmithKline, Neurosci Ctr Excellence Drug Discovery, Pain & Neuroexcitabil Discovery Performance Unit, Harlow CM19 5AW, Essex, England
关键词
Cannabinoid; CB2; CB1; SAR; CANNABINOID RECEPTOR; PHARMACOLOGY;
D O I
10.1016/j.bmcl.2009.10.041
中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
2-Amino-5-aryl-pyridines, exemplified by compound 1, had been identified as a synthetically tractable series of CB2 agonists from a high-throughput screen of the GlaxoSmithKline compound collection. Described herein are the results of an investigation of the structure-activity relationships (SAR) which led to the identification a number of potent and selective agonists. (C) 2009 Elsevier Ltd. All rights reserved.
引用
收藏
页码:6578 / 6581
页数:4
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