2-羟基-N,N-二甲基-3-{2-[[(R)-1-(5-甲基呋喃-2-基)丙基]氨基]-3,4-二氧代环丁-1-烯基氨基}苯甲酰胺（SCH 527123）的发现：一种强效的、口服生物可利用的CXCR2/CXCR1受体拮抗剂。
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.
作者信息
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
机构信息
Schering-Plough Research Institute, 2015 Galloping Hill Road, Kenilworth, NJ 07033, USA.
出版信息
J Med Chem. 2006 Dec 28;49(26):7603-6. doi: 10.1021/jm0609622.
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.
对先导环丁烯二酮3进行的构效关系研究，促成了4（SCH 527123）的发现，4是一种强效的、口服生物可利用的CXCR2/CXCR1受体拮抗剂，具有出色的基于细胞的活性。化合物4在大鼠中显示出良好的口服生物利用度，可能是治疗各种炎症性疾病的潜在治疗剂。
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