Optimization of 2-aminothiazole derivatives as CCR4 antagonists.
A series of 2-aminothiazole-derived antagonists of the CCR4 receptor has been synthesized and their affinity for the receptor evaluated using a [(125)I]TARC (CCL17) displacement assay. Optimization of these compounds for potency and pharmacokinetic properties led to the discovery of potent, orally bioavailable antagonists.
Wang
Xuemei
X
Amgen Inc., 1120 Veterans Boulevard, South San Francisco, CA 94080, USA.
Xu
Feng
F
Xu
Qingge
Q
Mahmud
Hossen
H
Houze
Jonathan
J
Zhu
Liusheng
L
Akerman
Michelle
M
Tonn
George
G
Tang
Liang
L
McMaster
Brian E
BE
Dairaghi
Daniel J
DJ
Schall
Thomas J
TJ
Collins
Tassie L
TL
Medina
Julio C
JC
D002460:Cell Line; D006801:Humans; D054398:Receptors, CCR4; D019707:Receptors, Chemokine / Q000037:antagonists & inhibitors*; D013844:Thiazoles / Q000493:pharmacokinetics / Q000494:pharmacology*
C515354:CCR4 protein, human; D054398:Receptors, CCR4; D019707:Receptors, Chemokine; D013844:Thiazoles