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Synthesis of New Bridgehead Substituted Azabicyclo-[2.2.1]heptane and -[3.3.1]nonane Derivatives as Potent and Selective alpha 7 Nicotinic Ligands

  作者 SLOWINSKI FRANCK; BEN AYAD OMAR; VACHE JULIEN; SAADY MOURAD; LECLERC ODILE; LOCHEAD ALISTAIR  
  选自 期刊  Organic Letters;  卷期  2010年12-21;  页码  5004-5007  
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[摘要]New azabicyclo[2.2.1]heptane and -[3.3.1]nonane derivatives containing a pyridinyl substituent at the bridgehead position have been synthesized via an efficient ten chemical steps pathway. Both chemical series were then evaluated in vitro for their affinity at alpha 7 nicotinic receptors revealing nanomolar potency with notably excellent selectivity over the alpha 4 beta 2 nicotinic subtype.

 
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