Discovery of 2-hydroxy-N,N-dimethyl-3-{2-[[(R)-1-(5-methylfuran-2-yl)propyl]amino]-3,4-dioxocyclobut-1-enylamino}benzamide (SCH 527123):: A potent, orally bioavailable CXCR2/CXCR1 receptor antagonist

被引：111
作者：
Dwyer, Michael P.
Yu, Younong
Chao, Jianping
Aki, Cynthia
Chao, Jianhua
Biju, Purakkattle
Girijavallabhan, Viyyoor
Rindgen, Diane
Bond, Richard
Mayer-Ezel, Rosemary
Jakway, James
Hipkin, R. William
Fossetta, James
Gonsiorek, Waldemar
Bian, Hong
Fan, Xuedong
Terminelli, Carol
Fine, Jay
Lundell, Daniel
Merritt, J. Robert
Rokosz, Laura L.
Kaiser, Bernd
Li, Ge
Wang, Wei
Stauffer, Tara
Ozgur, Lynne
Baldwin, John
Taveras, Arthur G.
机构：
[1] Schering Plough Res Inst, Kenilworth, NJ 07033 USA
[2] Pharmacopeia Drug Discovery Inc, Cranbury, NJ 08512 USA
来源：
JOURNAL OF MEDICINAL CHEMISTRY | 2006年 / 49卷 / 26期
关键词：
D O I：
10.1021/jm0609622
中图分类号：
R914 [药物化学];
学科分类号：
100701 ;
摘要：
Structure-activity studies on lead cyclobutenedione 3 led to the discovery of 4 (SCH 527123), a potent, orally bioavailable CXCR2/CXCR1 receptor antagonist with excellent cell-based activity. Compound 4 displayed good oral bioavailability in rat and may be a potential therapeutic agent for the treatment of various inflammatory diseases.
引用
收藏
页码：7603 / 7606
页数：4
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