Novel pyridine derivatives as potent and selective CB 2 cannabinoid receptor agonists

…, CJ LaBuda, M Koblish, B Brogdon, S Smith…

文献索引：Chu, Guo-Hua; Saeui, Christopher T.; Worm, Karin; Weaver, Damian G.; Goodman, Allan J.; Broadrup, Robert L.; Cassel, Joel A.; DeHaven, Robert N.; LaBuda, Christopher J.; Koblish, Michael; Brogdon, Bernice; Smith, Steve; Bourdonnec, Bertrand Le; Dolle, Roland E. Bioorganic and Medicinal Chemistry Letters, 2009 , vol. 19, # 20 p. 5931 - 5935

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被引用次数: 14

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.