Design and optimization of imidazole derivatives as potent CXCR3 antagonists.
A series of imidazole derivatives have been designed and optimized for CXCR3 antagonism, pharmacokinetic properties, and reduced formation of glutathione conjugates. Our efforts led to the discovery of potent CXCR3 antagonists with good pharmacokinetic properties. These compounds are useful tools for in vivo studies of CXCR3 function.
Amgen Inc. 1120 Veterans Boulevard, South San Francisco, CA 94080, USA.
Xiaohui
X
Du
Xiaoqi
X
Chen
Jeffrey T
JT
Mihalic
Jeffrey
J
Deignan
Jason
J
Duquette
An-Rong
AR
Li
Bryan
B
Lemon
Ji
J
Ma
Shichang
S
Miao
Karen
K
Ebsworth
Timothy J
TJ
Sullivan
George
G
Tonn
Tassie L
TL
Collins
Julio C
JC
Medina
D000818:Animals; D002851:Chromatography, High Pressure Liquid; D015195:Drug Design; D006801:Humans; D007093:Imidazoles / Q000737:chemistry* / Q000493:pharmacokinetics / Q000494:pharmacology*; D051379:Mice; D018345:Mice, Knockout; D051381:Rats; D054367:Receptors, CXCR3 / Q000037:antagonists & inhibitors* / Q000235:genetics / Q000502:physiology; D013329:Structure-Activity Relationship
C515188:Cxcr3 protein, mouse; D007093:Imidazoles; D054367:Receptors, CXCR3