Optimization of 2-aminothiazole derivatives as CCR4 antagonists

  • Bioorg Med Chem Lett. 2006 May 15;16(10):2800-3. doi: 10.1016/j.bmcl.2006.01.126.
Xuemei Wang  1 ,  Feng Xu ,  Qingge Xu ,  Hossen Mahmud ,  Jonathan Houze ,  Liusheng Zhu ,  Michelle Akerman ,  George Tonn ,  Liang Tang ,  Brian E McMaster ,  Daniel J Dairaghi ,  Thomas J Schall ,  Tassie L Collins ,  Julio C Medina
Affiliations
  • 1. Amgen Inc., 1120 Veterans Boulevard, South San Francisco, CA 94080, USA.
PMID: 16497499 DOI: 10.1016/j.bmcl.2006.01.126
Abstract

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.

Products