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From natural products to achiral drug prototypes: Potent thrombin inhibitors based on P-2/P-3 dihydropyrid-2-one core motifs

  作者 Hanessian, S; Therrien, E; Zhang, JB; van Otterlo, W; Xue, YF; Gustafsson, D; Nilsson, I; Fjellstrom, O  
  选自 期刊  Bioorganic & Medicinal Chemistry Letters;  卷期  2009年19-18;  页码  5429-5432  
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[摘要]A series of dihydropyrid-2-ones was synthesized and tested for inhibitory activity against serine protease enzymes. Moderate to low nanomolar inhibitory activities were obtained against thrombin and excellent selectivity against trypsin was observed. (C) 2009 Elsevier Ltd. All rights reserved.

 
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