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Rapid assessment of a novel series of selective CB2 agonists using parallel synthesis protocols: A Lipophilic Efficiency (LipE) analysis

  作者 Ryckmans, T; Edwards, MP; Horne, VA; Correia, AM; Owen, DR; Thompson, LR; Tran, I; Tutt, MF; Young, T  
  选自 期刊  Bioorganic & Medicinal Chemistry Letters;  卷期  2009年19-15;  页码  4406-4409  
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[摘要]A series of libraries were designed using the 1-(cyclopropylmethyl)-2-alkyl-4,5,6,7-tetrahydro-1H-imidazo[4,5-c] pyridin-5-ium templates 2a-b, and Sulfonamide derivatives 11a-n proved to be potent agonists of the CB2 receptor. Analysis of the Lipophilic Efficiency (LipE) of potent compounds provided new insight for the design of potent, metabolically stable CB2 agonists. (C) 2009 Elsevier Ltd. All rights reserved.

 
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