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N-benzyl-N-(pyrrolidin-3-yl) carboxamides as a new class of selective dual serotonin/noradrenaline reuptake inhibitors

  作者 Wakenhut, F; Fish, PV; Fray, MJ; Gurrell, I; Mills, JE; Stobie, A; Whitlock, GA  
  选自 期刊  Bioorganic & Medicinal Chemistry Letters;  卷期  2008年18-15;  页码  4308-4311  
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[摘要]The structure-activity relationship and the synthesis of novel N-benzyl-N-(pyrrolidin-3-yl)carboxamides as dual serotonin (5-HT) and noradrenaline (NA) monoamine reuptake inhibitors are described. Compounds such as 18 exhibited dual 5-HT and NA reuptake inhibition, good selectivity over dopamine (DA) reuptake inhibition and drug-like physicochemical properties consistent with CNS target space. Compound 18 was selected for further preclinical evaluation. (c) 2008 Elsevier Ltd. All rights reserved.

 
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