- 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.
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 chemistry (2006-12-22)
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 Fine, Daniel Lundell, J Robert Merritt, Laura L Rokosz, Bernd Kaiser, Ge Li, Wei Wang, Tara Stauffer, Lynne Ozgur, John Baldwin, Arthur G Taveras
PMID17181143
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.
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