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Bioorg Med Chem Lett. 2009 Feb 1;19(3):1022-5. doi: 10.1016/j.bmcl.2008.11.029. Epub 2008 Nov 14.

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

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Department of Chemistry, National Central University, 300 Jhong-Da Road, Jhongli City, Taoyuan, Taiwan.


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 (IC(50)<20 nM) are the triazoles containing benzyl amides. These triazoles also show excellent selectivity between CB1 and CB2 receptors (IC(50)>10 microM for CB2; CB2/CB1>1000).

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