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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Published inBioorganic & medicinal chemistry letters Vol. 19; no. 2; pp. 378 - 381
Main Authors Cole, Andrew G, Stauffer, Tara M, Rokosz, Laura L, Metzger, Axel, Dillard, Lawrence W, Zeng, Wenguang, Henderson, Ian
Format Journal Article
LanguageEnglish
Published England 15.01.2009
Subjects
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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Summary: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.
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ISSN:1464-3405
DOI:10.1016/j.bmcl.2008.11.066