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
Journal of Medicinal Chemistry2006Vol. 49(26), pp. 7603–7606
Citations Over TimeTop 10% of 2006 papers
Michael P. Dwyer, Younong Yu, Jianping Chao, Cynthia Aki, Jianhua Chao, Purakkattle Biju, Viyyoor Girijavallabhan, Diane Rindgen, Richard Bond, Rosemary Mayer-Ezel, James Jakway, R. William Hipkin, James Fossetta, Waldemar Gonsiorek, Hong Bian, Xuedong Fan, Carol Terminelli, Jay S. Fine, Daniel Lundell, J. Robert Merritt, Laura L. Rokosz, Bernd Kaiser, Ge Li, Wei Wang, Tara M. Stauffer, Lynne Ozgur, John J. Baldwin, Arthur G. Taveras
Abstract
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.
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