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.
Du
Xiaohui
X
Amgen Inc. 1120 Veterans Boulevard, South San Francisco, CA 94080, USA.
Chen
Xiaoqi
X
Mihalic
Jeffrey T
JT
Deignan
Jeffrey
J
Duquette
Jason
J
Li
An-Rong
AR
Lemon
Bryan
B
Ma
Ji
J
Miao
Shichang
S
Ebsworth
Karen
K
Sullivan
Timothy J
TJ
Tonn
George
G
Collins
Tassie L
TL
Medina
Julio C
JC
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