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Discovery of novel arylpyrazole series as potent and selective opioid receptor-like 1 (ORL1) antagonists

  作者 Kobayashi, K; Uchiyama, M; Ito, H; Takahashi, H; Yoshizumi, T; Sakoh, H; Nagatomi, Y; Asai, M; Miyazoe, H; Tsujita, T; Hirayama, M; Ozaki, S; Tani, T; Ishii, Y; Ohta, H; Okamoto, O  
  选自 期刊  Bioorganic & Medicinal Chemistry Letters;  卷期  2009年19-13;  页码  3627-3631  
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[摘要]The synthesis and biological evaluation of new potent opioid receptor-like 1 antagonists are presented. A structure-activity relationship (SAR) study of arylpyrazole lead compound 1 obtained from library screening identified compound 31, (1S, 3R)-N-{[1-(3-chloropyridin-2-yl)-5-(5-fluoro-6-methylpyridin-3-yl)-4-methyl-1H-pyrazol-3-yl]methyl}-3-fluorocyclopentanamine, which exhibits high intrinsic potency and selectivity against other opioid receptors and hERG potassium channel. (C) 2009 Elsevier Ltd. All rights reserved.

 
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