含3,4-二氨基环丁烯二酮的氟代烷基α侧链作为强效且口服生物可利用的CXCR2-CXCR1双重拮抗剂。
Fluoroalkyl alpha side chain containing 3,4-diamino-cyclobutenediones as potent and orally bioavailable CXCR2-CXCR1 dual antagonists.
作者信息
Biju Purakkattle, Taveras Arthur G, Dwyer Michael P, Yu Younong, Chao Jianhua, Hipkin R William, Fan Xuedong, Rindgen Diane, Fine Jay, Lundell Daniel
机构信息
Schering-Plough Research Institute, Kenilworth, NJ 07033, USA.
出版信息
Bioorg Med Chem Lett. 2009 Mar 1;19(5):1431-3. doi: 10.1016/j.bmcl.2009.01.033. Epub 2009 Jan 15.
PMID:19196511
Abstract
A series of potent and orally bioavailable 3,4-diaminocyclobutenediones with various fluoroalkyl groups as alpha side chain were prepared and found to show significant improvements in the binding affinities towards both CXCR2 and CXCR1 receptors.
摘要
制备了一系列具有不同氟代烷基作为α侧链的强效且口服生物可利用的3,4-二氨基环丁烯二酮，并发现它们对CXCR2和CXCR1受体的结合亲和力有显著提高。
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