Synthesis of 2-amino-5-benzoyl-4-(2-furyl)thiazoles as adenosine A(2A) receptor antagonists

The discovery and synthesis of a series of 2-amino-5-benzoyl-4-(2-furyl)thiazoles as adenosine A(2A) receptor antagonists from a small-molecule combinatorial library using a high-throughput radioligand-binding assay is described. Antagonists were further characterized in the A(2A) binding assay and...

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Veröffentlicht in:	Bioorganic & medicinal chemistry letters 2009-01, Vol.19 (2), p.378-381
Hauptverfasser:	Cole, Andrew G, Stauffer, Tara M, Rokosz, Laura L, Metzger, Axel, Dillard, Lawrence W, Zeng, Wenguang, Henderson, Ian
Format:	Artikel
Sprache:	eng
Schlagworte:	Alkylation Cell Line Combinatorial Chemistry Techniques Drug Discovery Humans Purinergic P1 Receptor Antagonists Radioligand Assay Receptors, Purinergic P1 - metabolism Thiazoles - chemical synthesis Thiazoles - metabolism Thiazoles - pharmacology
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Beschreibung
Zusammenfassung:	The discovery and synthesis of a series of 2-amino-5-benzoyl-4-(2-furyl)thiazoles as adenosine A(2A) receptor antagonists from a small-molecule combinatorial library using a high-throughput radioligand-binding assay is described. Antagonists were further characterized in the A(2A) binding assay and an A(1) selectivity assay. Selected examples exhibited excellent affinity for A(2A) and good selectivity versus the A(1) receptor.
ISSN:	1464-3405
DOI:	10.1016/j.bmcl.2008.11.066