Novel pyridine derivatives as potent and selective CB2 cannabinoid receptor agonists

被引：14

作者：

Chu, Guo-Hua ^{[1
]}

Saeui, Christopher T. ^{[1
]}

Worm, Karin ^{[1
]}

Weaver, Damian G. ^{[1
]}

Goodman, Allan J. ^{[1
]}

Broadrup, Robert L. ^{[1
]}

Cassel, Joel A. ^{[2
]}

DeHaven, Robert N. ^{[2
]}

LaBuda, Christopher J. ^{[2
]}

Koblish, Michael ^{[2
]}

Brogdon, Bernice ^{[3
]}

Smith, Steve ^{[3
]}

Le Bourdonnec, Bertrand ^{[1
]}

Dolle, Roland E. ^{[1
]}

机构：

[1] Adolor Corp, Dept Chem, Exton, PA 19341 USA

[2] Adolor Corp, Dept Pharmacol, Exton, PA 19341 USA

[3] Adolor Corp, Dept DMPK, Exton, PA 19341 USA

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2009年 / 19卷 / 20期

关键词：

Cannabinoid receptors; Selective CB2 agonists; Pain; Pyridine derivatives; PAIN; BINDING; ACTIVATION; DISCOVERY; RAT;

D O I：

10.1016/j.bmcl.2009.08.063

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

Replacement of the phenyl ring in our previous ( morpholinomethyl) aniline carboxamide cannabinoid receptor ligands with a pyridine ring led to the discovery of a novel chemical series of CB2 ligands. Compound 3, that is, 2,2-dimethyl-N-(5-methyl-4-(morpholinomethyl)pyridin-2-yl)butanamide was identified as a potent and selective CB2 agonist exhibiting in vivo efficacy after oral administration in a rat model of neuropathic pain. (C) 2009 Elsevier Ltd. All rights reserved.

引用

页码：5931 / 5935

页数：5

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