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

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題名:	1,2,3-Triazole derivatives as new cannabinoid CB1 receptor antagonists
作者:	Hou,DR;Alam,S;Kuan,TC;Ramanathan,M;Lin,TP;Hung,MS
貢獻者:	中央大學
關鍵詞:	MOLECULAR MODELING INVESTIGATIONS;BIOLOGICAL-PROPERTIES;INVERSE AGONISTS;LATEST ADVANCES;POTENT;DISCOVERY;OBESITY;3;4-DIARYLPYRAZOLINES;PHARMACOLOGY;SR141716A
日期:	2009
上傳時間:	2010-06-29 19:44:38 (UTC+8)
出版者:	化學研究所
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 mu M for CB2; CB2/CB1 > 1000). (C) 2008 Elsevier Ltd. All rights reserved.
關聯:	BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
顯示於類別:	[化學研究所] 期刊論文

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