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Discovery of dehydro-oxopiperazine acetamides as novel bradykinin B1 receptor antagonists with enhanced in vitro potency

  作者 Qian, WY; Chen, JJ; Human, J; Aya, T; Zhu, JW; Biswas, K; Peterkin, T; Hungate, RW; Arik, L; Johnson, E; Kumar, G; Joseph, S; Jona, J; Guo, HX; Wu, ZF  
  选自 期刊  Bioorganic & Medicinal Chemistry Letters;  卷期  2012年22-2;  页码  1061-1067  
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[摘要]In a series of bradykinin B1 antagonists, we discovered that replacement of oxopiperazine acetamides with dehydro-oxopiperazine acetamides provided compounds with enhanced activity against the B1 receptor. The synthesis and SAR leading to potent analogs with reduced molecular weight will be discussed. (C) 2011 Published by Elsevier Ltd.

 
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