Title of article
Synthesis and structure–activity relationships of 3,4-diaminocyclobut-3-ene-1,2-dione CXCR2 antagonists
Author/Authors
J. Robert Merritt، نويسنده , , Laura L. Rokosz، نويسنده , , Kingsley H. Nelson Jr.، نويسنده , , Bernd Kaiser، نويسنده , , Wei Wang، نويسنده , , Tara M. Stauffer، نويسنده , , Lynne E. Ozgur، نويسنده , , Adriane Schilling، نويسنده , , Ge Li، نويسنده , , John J. Baldwin، نويسنده , , Arthur G. Taveras، نويسنده , , Michael P. Dwyer، نويسنده , , Jianping Chao، نويسنده ,
Issue Information
روزنامه با شماره پیاپی سال 2006
Pages
4
From page
4107
To page
4110
Abstract
A novel series of 3,4-diaminocyclobut-3-ene-1,2-diones was prepared and found to show potent inhibitory activity of CXCR2 binding and IL-8-mediated chemotaxis of a CXCR2-expressing cell line. Microsome stability and Caco2 studies were subsequently used to show that compounds of this chemotype are predicted to have good oral bioavailability and are thus suitable for pharmaceutical development.
Keywords
CXCR2 , Cyclobutenedione , CXCR1 , 3 , Squarate , 4-Diaminocyclobut-3-ene-1 , 2-dione , IL-8 , CXCL8 , neutrophil , chemokine
Journal title
Bioorganic & Medicinal Chemistry Letters
Serial Year
2006
Journal title
Bioorganic & Medicinal Chemistry Letters
Record number
797145
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