Diaminocyclobutenediones as potent and orally bioavailable CXCR2 receptor antagonists: SAR in the phenolic amide region.
A series of potent and orally bioavailable 3,4-diaminocyclobutenediones with various amide modifications and substitution on the left side phenyl ring were prepared and found to show significant inhibitory activities towards both CXCR2 and CXCR1 receptors.
Aki
Cynthia
C
Department of Chemical Research, Schering-Plough Research Institute, 2015 Galloping Hill Road, Kenilworth, NJ 07033, USA.
Chao
Jianping
J
Ferreira
Johan A
JA
Dwyer
Michael P
MP
Yu
Younong
Y
Chao
Jianhua
J
Merritt
Robert J
RJ
Lai
Gaifa
G
Wu
Minglang
M
Hipkin
R William
RW
Fan
Xuedong
X
Gonsiorek
Waldemar
W
Fosseta
James
J
Rindgen
Diane
D
Fine
Jay
J
Lundell
Daniel
D
Taveras
Arthur G
AG
Biju
Purakkattle
P
D000284:Administration, Oral; D000577:Amides / Q000737:chemistry*; D000818:Animals; D019540:Area Under Curve; D002626:Chemistry, Pharmaceutical / Q000379:methods; D003503:Cyclobutanes / Q000138:chemical synthesis* / Q000494:pharmacology; D003959:Diamines / Q000138:chemical synthesis* / Q000494:pharmacology; D015195:Drug Design; D006801:Humans; D007249:Inflammation; D007700:Kinetics; D008956:Models, Chemical; D019800:Phenol / Q000737:chemistry*; D051381:Rats; D023062:Receptors, Interleukin-8A / Q000037:antagonists & inhibitors*; D023063:Receptors, Interleukin-8B / Q000037:antagonists & inhibitors*; D013329:Structure-Activity Relationship
D000577:Amides; D003503:Cyclobutanes; D003959:Diamines; D023062:Receptors, Interleukin-8A; D023063:Receptors, Interleukin-8B; D019800:Phenol