Synthesis and structure–activity relationships of new disubstituted phenyl-containing 3,4-diamino-3-cyclobutene-1,2-diones as CXCR2 receptor antagonists
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- 作者：Gaifa Lai ; J. Robert Merritt ; Zhenmin He ; Daming Feng ; Jianhua Chao ; Michael F. Czarniecki ; Laura L. Rokosz ; Tara M. Stauffer ; Diane Rindgen ; Arthur G. Taveras
- 关键词：CXCR2 receptor ; Antagonists ; Cyclobutenediones ; Synthesis ; Structure– ; activity relationships
- 刊名：Bioorganic and Medicinal Chemistry Letters
- 出版年：2008
- 出版时间：15 March 2008
- 年：2008
- 卷：18
- 期：6
- 页码：1864-1868
- 全文大小：151 K
文摘
A series of 3,4- and 3,5-disubstituted phenyl-containing cyclobutenedione analogues were synthesized and evaluated as CXCR2 receptor antagonists. Variations in the disubstitution pattern of the phenyl ring afforded new compounds with potent CXCR2 binding affinity in the low nanomolar ranges. Moreover, two potent compounds 19 and 26 exhibited good oral pharmacokinetic profiles.