Title of article
Synthesis and structure–activity relationships of new disubstituted phenyl-containing 3,4-diamino-3-cyclobutene-1,2-diones as CXCR2 receptor antagonists
Author/Authors
Gaifa Lai، نويسنده , , J. Robert Merritt، نويسنده , , Zhenmin He، نويسنده , , Daming Feng، نويسنده , , Jianhua Chao، نويسنده , , Michael F. Czarniecki، نويسنده , , Laura L. Rokosz، نويسنده , , Tara M. Stauffer، نويسنده , , Diane Rindgen، نويسنده , , Arthur G. Taveras، نويسنده ,
Issue Information
روزنامه با شماره پیاپی سال 2008
Pages
5
From page
1864
To page
1868
Abstract
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.
Keywords
Cyclobutenediones , Antagonists , synthesis , Structure–activity relationships , CXCR2 receptor
Journal title
Bioorganic & Medicinal Chemistry Letters
Serial Year
2008
Journal title
Bioorganic & Medicinal Chemistry Letters
Record number
799262
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