The development of new isoxazolone based inhibitors of tumor necrosis factor-alpha (TNF-α) production

被引:61
作者
Laughlin, SK [1 ]
Clark, MP [1 ]
Djung, JF [1 ]
Golebiowski, A [1 ]
Brugel, TA [1 ]
Sabat, M [1 ]
Bookland, RG [1 ]
Laufersweiler, MJ [1 ]
VanRens, JC [1 ]
Townes, JA [1 ]
De, B [1 ]
Hsieh, LC [1 ]
Xu, SC [1 ]
Walter, RL [1 ]
Mekel, MJ [1 ]
Janusz, MJ [1 ]
机构
[1] Procter & Gamble Pharmaceut, Hlth Care Res Ctr, Mason, OH 45040 USA
关键词
D O I
10.1016/j.bmcl.2005.02.066
中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
4-Aryl-3-pyridyl and 4-aryl-3-pyrimidinyl based tumor necrosis factor-alpha (TNF-alpha) inhibitors, which contain a novel isoxazolone five-membered heterocyclic core are described. Many showed sub-micromolar activity against lipopolysaccharide-induced TNF-alpha production. (c) 2005 Published by Elsevier Ltd.
引用
收藏
页码:2399 / 2403
页数:5
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