Optimization of 2-aminothiazole derivatives as CCR4 antagonists.

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

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.

Afiliação

Wang X; Amgen Inc., 1120 Veterans Boulevard, South San Francisco, CA 94080, USA.

Bioorg Med Chem Lett ; 16(10): 2800-3, 2006 May 15.

Article em En | MEDLINE | ID: mdl-16497499

ABSTRACT

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.

Assuntos

Receptores de Quimiocinas/antagonistas & inibidores; Tiazóis/farmacologia; Linhagem Celular; Humanos; Receptores CCR4; Tiazóis/farmacocinética

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Base de dados: MEDLINE Assunto principal: Tiazóis / Receptores de Quimiocinas Limite: Humans Idioma: En Ano de publicação: 2006 Tipo de documento: Article

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Imprimir

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PubMed Links

Base de dados: MEDLINE Assunto principal: Tiazóis / Receptores de Quimiocinas Limite: Humans Idioma: En Ano de publicação: 2006 Tipo de documento: Article