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1,2,3-Triazole derivatives as new cannabinoid CB1 receptor antagonists

1,2,3-Triazole derivatives as new cannabinoid CB1 receptor antagonists

  1. ThirdEyeFloond
    Bioorganic & Medicinal Chemistry Letters
    Volume 19, Issue 3, 1 February 2009, Pages 1022-1025

    Duen-Ren Hou, Safiul Alam, Ting-Chun Kuan, Mani Ramanathan, Tsung-Pang Lin and Ming-Shiu Hung


    This letter reports the new entry of novel 1,2,3-triazole derivatives as CB1 receptor antagonists. The design, synthesis and biological evaluation of N1 and N2 substituted 1,2,3-trizoles are described. The N2 substituted, symmetrical 1,2,3-triazoles are more potent ligands than the unsymmetrical analogues. The in vitro activity of these triazoles is further improved by inserting a methylene group between the central core and the carbonyl side chain. The most potent antagonists prepared in this series (IC50 < 20 nM) are the triazoles containing benzyl amides. These triazoles also show excellent selectivity between CB1 and CB2 receptors (IC50 > 10 μM for CB2; CB2/CB1 > 1000).