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Discovery of selective PDE4B inhibitors

  作者 Naganuma, K; Omura, A; Maekawara, N; Saitoh, M; Ohkawa, N; Kubota, T; Nagumo, H; Kodama, T; Takemura, M; Ohtsuka, Y; Nakamura, J; Tsujita, R; Kawasaki, K; Yokoi, H; Kawanishi, M  
  选自 期刊  Bioorganic & Medicinal Chemistry Letters;  卷期  2009年19-12;  页码  3174-3176  
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[摘要]In this study the first PDE4B selective inhibitor is described. Optimization of lead 2-arylpyrimidine derivatives afforded a series of potent PDE4B inhibitors with >100-fold selectivity over the PDE4D isozyme. With a good pharmacokinetic profile, a selected compound exhibited potent anti-inflammatory effects in vivo and showed less emesis compared with Cilomilast. (C) 2009 Elsevier Ltd. All rights reserved.

 
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