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Pyrazole-based sulfonamide and sulfamides as potent inhibitors of mammalian 15-lipoxygenase

  作者 Ngu, K; Weinstein, DS; Liu, W; Langevine, C; Combs, DW; Zhuang, SB; Chen, X; Madsen, CS; Harper, TW; Ahmad, S; Robl, JA  
  选自 期刊  Bioorganic & Medicinal Chemistry Letters;  卷期  2011年21-14;  页码  4141-4145  
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[摘要]A series of inhibitors of mammalian 15-lipoxygenase (15-LO) based on a 3,4,5-tri-substituted pyrazole scaffold is described. Replacement of a sulfonamide functionality in the lead series with a sulfamide group resulted in improved physicochemical properties generating analogs with enhanced inhibition in cell-based and whole blood assays. (C) 2011 Elsevier Ltd. All rights reserved.

 
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