國家衛生研究院 NHRI:Item 3990099045/3513
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    题名: 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
    贡献者: Division of Biotechnology and Pharmaceutical Research
    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).
    日期: 2009-02-01
    關聯: Bioorganic and Medicinal Chemistry Letters. 2009 Feb 1;19(3):1022-1025.
    Link to: http://dx.doi.org/10.1016/j.bmcl.2008.11.029
    JIF/Ranking 2023: http://gateway.webofknowledge.com/gateway/Gateway.cgi?GWVersion=2&SrcAuth=NHRI&SrcApp=NHRI_IR&KeyISSN=0960-894X&DestApp=IC2JCR
    Cited Times(WOS): https://www.webofscience.com/wos/woscc/full-record/WOS:000262707000103
    Cited Times(Scopus): http://www.scopus.com/inward/record.url?partnerID=HzOxMe3b&scp=58549117673
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