@article{1f7056f194074247a360d31761b443b1,
title = "1,2,3-Triazole derivatives as new cannabinoid CB1 receptor antagonists",
abstract = "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).",
keywords = "Cannabinoid, Obesity, Triazole",
author = "Hou, {Duen Ren} and Safiul Alam and Kuan, {Ting Chun} and Mani Ramanathan and Lin, {Tsung Pang} and Hung, {Ming Shiu}",
note = "Funding Information: This research was supported by the National Science Council (NSC 95-2323-B-007-005, NSC 96-2323-B-007-001 and NSC 95-2133-M-008-007-MY3), and National Health Research Institutes (NHRI), Taiwan, ROC. We are grateful to Ms. Ping-Yu Lin at the Institute of Chemistry, Academia Sinica, Ms. Wen-Chi Hsiao at NHRI, and Valuable Instrument Center in National Central University for obtaining mass analysis. ",
year = "2009",
month = feb,
day = "1",
doi = "10.1016/j.bmcl.2008.11.029",
language = "???core.languages.en_GB???",
volume = "19",
pages = "1022--1025",
journal = "Bioorganic and Medicinal Chemistry Letters",
issn = "0960-894X",
number = "3",
}