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 [125I]TARC (CCL17) displacement assay. Optimization of these compounds for potency and pharmacokinetic properties led to the discovery of potent, orally bio...

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Veröffentlicht in:	Bioorganic & medicinal chemistry letters 2006-05, Vol.16 (10), p.2800-2803
Hauptverfasser:	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.
Format:	Artikel
Sprache:	eng
Schlagworte:	Biological and medical sciences CCL17 CCL22 CCR4 Cell Line Chemokine Chemokine receptor GPCR Humans MDC Medical sciences Miscellaneous Pharmacology. Drug treatments Receptors, CCR4 Receptors, Chemokine - antagonists & inhibitors TARC Thiazoles - pharmacokinetics Thiazoles - pharmacology
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Beschreibung
Zusammenfassung:	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. 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.
ISSN:	0960-894X 1464-3405
DOI:	10.1016/j.bmcl.2006.01.126