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Oxadiazole-diarylpyrazole 4-carboxamides as cannabinoid CB1 receptor ligands

Oxadiazole-diarylpyrazole 4-carboxamides as cannabinoid CB1 receptor ligands

  1. ThirdEyeFloond
    Bioorganic & Medicinal Chemistry Letters
    Volume 19, Issue 7, 1 April 2009, Pages 1899-1902

    Suk Ho Lee, Hee Jeong Seo, Min Ju Kim, Suk Youn Kang, Kwang-Seop Song, Sung-Han Lee, Myung Eun Jung, Jeongmin Kim and Jinhwa Lee

    Cannabinoid CB-1 receptors have been the focus of extensive studies since the first clinical results of rimonabant (SR141716) for the treatment of obesity and obesity-related metabolic disorders were reported in 2001. To further evaluate the properties of CB receptors, we have designed and efficiently prepared a series of oxadiazole-diarylpyrazole 4-carboxamides. Six of the new compounds which displayed high in vitro CB1 binding affinities were assayed for binding to CB2 receptor. Noticeably, 5-(4-bromophenyl)-3-(5-tert-butyl-1,3,4-oxadiazol-2-yl)-1-(2,4-dichlorophenyl)-N-phenyl-1H-pyrazole-4-carboxamide (12q) and 5-(4-bromophenyl)-3-(5-tert-butyl-1,3,4-oxadiazol-2-yl)-1-(2,4-dichlorophenyl)-N-(pyridin-2-yl)-1H-pyrazole-4-carboxamide (12r) demonstrated good binding affinity and decent selectivity for CB1 receptor (IC50 = 1.35 nM, CB2/CB1 = 286 for 12q; IC50 = 1.46 nM, CB2/CB1 = 256 for 12r).
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