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Pyrazoloquinolines as PDE10A inhibitors: Discovery of a tool compound

  作者 McElroy, WT; Tan, Z; Basu, K; Yang, SW; Smotryski, J; Ho, GD; Tulshian, D; Greenlee, WJ; Mullins, D; Guzzi, M; Zhang, XP; Bleickardt, C; Hodgson, R  
  选自 期刊  Bioorganic & Medicinal Chemistry Letters;  卷期  2012年22-3;  页码  1335-1339  
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[摘要]A series of pyrazoloquinolines, possessing (hetero)arylhydroxymethyl substituents at the quinoline C-4 position were evaluated as PDE10A inhibitors. Among these, methylpyrimidyl analogue 15 was identified as having good rodent and monkey exposure, and a MED of 10 mg/kg in an in vivo model. (C) 2011 Elsevier Ltd. All rights reserved.

 
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