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

被引：30
|
作者：
Ngu, Khehyong [1 ]
Weinstein, David S. [1 ]
Liu, Wen [1 ]
Langevine, Charles [1 ]
Combs, Donald W. [1 ]
Zhuang, Shaobin [1 ]
Chen, Xing [1 ]
Madsen, Cort S. [1 ]
Harper, Timothy W. [1 ]
Ahmad, Saleem [1 ]
Robl, Jeffrey A. [1 ]
机构：
[1] Bristol Myers Squibb Co, Res & Dev, Princeton, NJ 08543 USA
来源：
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2011年 / 21卷 / 14期
关键词：
15-Lipoxygenase; Inhibitors; Pyrazole; Sulfonamides; Sulfamides; Arachidonic acid; Linoleic acid; LIPOXYGENASE INHIBITORS; SELECTIVE INHIBITORS; CANCER CELLS; 12-LIPOXYGENASE; 12/15-LIPOXYGENASE; DERIVATIVES; DISCOVERY; DISEASE; DESIGN; ENZYME;
D O I：
10.1016/j.bmcl.2011.05.107
中图分类号：
R914 [药物化学];
学科分类号：
100701 ;
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.
引用
收藏
页码：4141 / 4145
页数：5
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