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Structure-activity relationships of 3-substituted N-benzhydryl-nortropane analogs as nociceptin receptor ligands for the treatment of cough

  作者 Yang, SW; Ho, G; Tulshian, D; Greenlee, WJ; Fernandez, X; McLeod, RL; Eckel, S; Anthes, J  
  选自 期刊  Bioorganic & Medicinal Chemistry Letters;  卷期  2008年18-24;  页码  6340-6343  
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[摘要]A series of 3-axial-aminomethyl-N-benzhydryl-nortropane analogs have been synthesized and identified to bind to the nociceptin receptor with high affinity. Many of these analogs showed high binding selectivity over classic opioid receptors such as l receptor. The synthesis and structure-activity relationships around the C-3 nortropane substitution are described. Selected compounds with potent oral antitussive activity in the guinea pig model are disclosed. (C) 2008 Elsevier Ltd. All rights reserved.

 
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