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 ,
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
