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The discovery of azepane sulfonamides as potent 11 beta-HSD1 inhibitors

  作者 Neelamkavil, SF; Boyle, CD; Chackalamannil, S; Greenlee, WJ; Zhang, LL; Terracina, G  
  选自 期刊  Bioorganic & Medicinal Chemistry Letters;  卷期  2009年19-16;  页码  4563-4565  
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[摘要]Discovery of a series of azepine sulfonamides as potent inhibitors of 11 beta-hydroxysteroid dehydrogenase type 1 (11 beta-HSD1) is described. SAR studies at the 4-position of the azepane ring have resulted in the discovery of a very potent compound 30 which has an 11 beta-HSD1 IC50 of 3.0 nM. (C) 2009 Elsevier Ltd. All rights reserved.

 
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