Literature DB >> 19646869

Discovery of N-(3-(morpholinomethyl)-phenyl)-amides as potent and selective CB2 agonists.

Karin Worm1, Damian G Weaver, Rosalyn C Green, Christopher T Saeui, Doreen-Marie S Dulay, William M Barker, Joel A Cassel, Gabriel J Stabley, Robert N DeHaven, Christopher J LaBuda, Michael Koblish, Bernice L Brogdon, Steven A Smith, Roland E Dolle.   

Abstract

Recently sulfamoyl benzamides were identified as a novel series of cannabinoid receptor ligands. Replacing the sulfonamide functionality and reversing the original carboxamide bond led to the discovery of N-(3-(morpholinomethyl)-phenyl)-amides as potent and selective CB(2) agonists. Selective CB(2) agonist 31 (K(i)=2.7; CB(1)/CB(2)=190) displayed robust activity in a rodent model of postoperative pain.

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Year:  2009        PMID: 19646869     DOI: 10.1016/j.bmcl.2009.07.057

Source DB:  PubMed          Journal:  Bioorg Med Chem Lett        ISSN: 0960-894X            Impact factor:   2.823


  2 in total

Review 1.  Latest advances in novel cannabinoid CB(2) ligands for drug abuse and their therapeutic potential.

Authors:  Peng Yang; Lirong Wang; Xiang-Qun Xie
Journal:  Future Med Chem       Date:  2012-02       Impact factor: 3.808

2.  Matrix metalloproteinase expression and molecular interaction network analysis in gastric cancer.

Authors:  Jianting Xu; Changyong E; Yongfang Yao; Shuangchun Ren; Guoqing Wang; Haofan Jin
Journal:  Oncol Lett       Date:  2016-08-16       Impact factor: 2.967

  2 in total

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