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Aryl sulfones as novel Bradykinin B1 receptor antagonists for treatment of chronic pain

  作者 Biswas, K; Aya, T; Qian, WY; Peterkin, TAN; Chen, JJ; Human, J; Hungate, RW; Kumar, G; Arik, L; Lester-Zeiner, D; Biddlecome, G; Manning, BH; Sun, H; Dong, H; Huang, M; Loeloff, R; Johnson, EJ; Askew, BC  
  选自 期刊  Bioorganic & Medicinal Chemistry Letters;  卷期  2008年18-17;  页码  4764-4769  
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[摘要]We report the development of aryl sulfones as Bradykinin B1 receptor antagonists. Variation of the linker region identified diol 23 as a potent B1 antagonist, while modi. cations of the aryl moiety led to compound 26, both of which were efficacious in rabbit biochemical challenge and pain models. (C) 2008 Elsevier Ltd. All rights reserved.

 
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