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Pyrazolo[1,5-a]pyrimidine-based inhibitors of HCV polymerase

  作者 Popovici-Muller, J; Shipps, GW; Rosner, KE; Deng, YQ; Wang, T; Curran, PJ; Brown, MA; Siddiqui, MA; Cooper, AB; Duca, J; Cable, M; Girijavallabhan, V  
  选自 期刊  Bioorganic & Medicinal Chemistry Letters;  卷期  2009年19-22;  页码  6331-6336  
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[摘要]The present paper describes a novel series of HCV RNA polymerase inhibitors based on a pyrazolo[1,5-a]pyrimidine scaffold bearing hydrophobic groups and an acidic functionality. Several compounds were optimized to low nanomolar potencies in a biochemical RdRp assay. SAR trends clearly reveal a stringent preference for a cyclohexyl group as one of the hydrophobes, and improved activities for carboxylic acid derivatives. (C) 2009 Elsevier Ltd. All rights reserved.

 
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