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
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- 作者：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 ; Ja
- 刊名：Journal of Medicinal Chemistry
- 出版年：2006
- 出版时间：December 28, 2006
- 年：2006
- 卷：49
- 期：26
- 页码：7603 - 7606
- 全文大小：71K
- 年卷期：v.49,no.26(December 28, 2006)
- ISSN：1520-4804
文摘
Structure-activity studies on lead cyclobutenedione 3 ledto the discovery of 4 (SCH 527123), a potent, orally bioavailableCXCR2/CXCR1 receptor antagonist with excellent cell-based activity.Compound 4 displayed good oral bioavailability in rat and may be apotential therapeutic agent for the treatment of various inflammatorydiseases.