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

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

研究成果: 雜誌貢獻期刊論文同行評審

49 引文 斯高帕斯(Scopus)

摘要

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).

原文???core.languages.en_GB???
頁(從 - 到)1022-1025
頁數4
期刊Bioorganic and Medicinal Chemistry Letters
19
發行號3
DOIs
出版狀態已出版 - 1 2月 2009

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