Fluoroalkyl alpha side chain containing 3,4-diamino-cyclobutenediones as potent and orally bioavailable CXCR2-CXCR1 dual antagonists.
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.
Biju
Purakkattle
P
Schering-Plough Research Institute, Kenilworth, NJ 07033, USA.
Taveras
Arthur G
AG
Dwyer
Michael P
MP
Yu
Younong
Y
Chao
Jianhua
J
Hipkin
R William
RW
Fan
Xuedong
X
Rindgen
Diane
D
Fine
Jay
J
Lundell
Daniel
D
D000284:Administration, Oral; D000818:Animals; D001665:Binding Sites; D003503:Cyclobutanes / Q000008:administration & dosage / Q000138:chemical synthesis* / Q000378:metabolism; D011485:Protein Binding; D051381:Rats; D023062:Receptors, Interleukin-8A / Q000037:antagonists & inhibitors* / Q000378:metabolism; D023063:Receptors, Interleukin-8B / Q000037:antagonists & inhibitors* / Q000378:metabolism
D003503:Cyclobutanes; D023062:Receptors, Interleukin-8A; D023063:Receptors, Interleukin-8B