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.
Amgen Inc., 1120 Veterans Boulevard, South San Francisco, CA 94080, USA.
Xuemei
X
Wang
Feng
F
Xu
Qingge
Q
Xu
Hossen
H
Mahmud
Jonathan
J
Houze
Liusheng
L
Zhu
Michelle
M
Akerman
George
G
Tonn
Liang
L
Tang
Brian E
BE
McMaster
Daniel J
DJ
Dairaghi
Thomas J
TJ
Schall
Tassie L
TL
Collins
Julio C
JC
Medina
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