2. Academic Validation
  3. Optimization of 2-aminothiazole derivatives as CCR4 antagonists

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

Affiliation

  • 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.

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