Pyridine-3-carboxamides as novel CB2 agonists for analgesia

被引：23

作者：

Mitchell, William L. ^{[1
]}

Giblin, Gerard M. P. ^{[1
]}

Naylor, Alan ^{[1
]}

Eatherton, Andrew J. ^{[1
]}

Slingsby, Brian P. ^{[1
]}

Rawlings, Anthony D. ^{[1
]}

Jandu, Karamjit S. ^{[1
]}

Haslam, Carl P. ^{[1
]}

Brown, Andrew J. ^{[1
]}

Goldsmith, Paul ^{[1
]}

Clayton, Nick M. ^{[1
]}

Wilson, Alex W. ^{[1
]}

Chessell, Iain P. ^{[1
]}

Green, Richard H. ^{[1
]}

Whittington, Andrew R. ^{[1
]}

Wall, Ian D. ^{[1
]}

机构：

[1] GlaxoSmithKline PLC, Neurosci Ctr Excellence Drug Discovery, Harlow CM19 5AW, Essex, England

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2009年 / 19卷 / 01期

关键词：

Analgesia; CB2; agonist; Inflammatory pain; Cannabinoid receptors; GW842166X; Structure-activity-relationships; Pharmacokinetics; Solubility; Weinreb reaction; Cytochrome P450; in vitro clearance; Hyperalgesia; Complete Freund's Adjuvant; Bioavailability; 4-Cyclopropyl-6-[(2,4-dichlorophenyl)amino]-N-[(tetrahydro-2H-pyran-4-yl)methyl]-3-pyridinecarboxamide; CANNABINOID RECEPTOR AGONISTS; NORADRENALINE RELEASE; INFLAMMATORY PAIN; IN-VITRO; INHIBITION; PYRIDINE; RELIEF; MODELS; SYSTEM; BRAIN;

D O I：

10.1016/j.bmcl.2008.10.118

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

We describe herein the medicinal chemistry approach which led to the discovery of a novel pyridine-3-carboxamide series of CB(2) receptor agonists. The SAR of this new template was evaluated and culminated in the identification of analogue 14a which demonstrated efficacy in an in vivo model of inflammatory pain. (C) 2008 Elsevier Ltd. All rights reserved.

引用

页码：259 / 263

页数：5

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