Optimization of 2-aminothiazole derivatives as CCR4 antagonists

…, J Houze, L Zhu, M Akerman, G Tonn, L Tang…

Index: Wang, Xuemei; Xu, Feng; Xu, Qingge; Mahmud, Hossen; Houze, Jonathan; Zhu, Liusheng; Akerman, Michelle; Tonn, George; Tang, Liang; McMaster, Brian E.; Dairaghi, Daniel J.; Schall, Thomas J.; Collins, Tassie L.; Medina, Julio C. Bioorganic and Medicinal Chemistry Letters, 2006 , vol. 16, # 10 p. 2800 - 2803

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Citation Number: 35

Abstract

A series of 2-aminothiazole-derived antagonists of the CCR4 receptor has been synthesized and their affinity for the receptor evaluated using a [125I] TARC (CCL17) displacement assay. Optimization of these compounds for potency and pharmacokinetic properties led to the discovery of potent, orally bioavailable antagonists.