Synthesis of 2-amino-5-benzoyl-4-(2-furyl)thiazoles as adenosine A2A receptor antagonists

The discovery and synthesis of a series of 2-amino-5-benzoyl-4-(2-furyl)thiazoles as adenosine A2A receptor antagonists from a small-molecule combinatorial library using a high-throughput radioligand-binding assay is described. Antagonists were further characterized in the A2A binding assay and an A...

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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, WENGUANG ZENG, HENDERSON, Ian
Format Journal Article
LanguageEnglish
Published Amsterdam Elsevier 15.01.2009
Subjects
Biological and medical sciences
Medical sciences
Neuropharmacology
Neurotransmitters. Neurotransmission. Receptors
Peptidergic system (neuropeptide, opioid peptide, opiates...). Adenosinergic and purinergic systems
Pharmacology. Drug treatments
Sulfur nitrogen heterocycle
Adenosine
Parkinson's disease
Aminothiazole
Thiazole derivatives
Furan derivatives
Combinatorial chemistry
Selectivity
Oxygen heterocycle
ECLiPS
Ketone
A2A adenosine receptor
G protein coupled receptor
Affinity
GPCR
Antagonist
Chemical synthesis
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Summary:The discovery and synthesis of a series of 2-amino-5-benzoyl-4-(2-furyl)thiazoles as adenosine A2A receptor antagonists from a small-molecule combinatorial library using a high-throughput radioligand-binding assay is described. Antagonists were further characterized in the A2A binding assay and an A1 selectivity assay. Selected examples exhibited excellent affinity for A2A and good selectivity versus the A1 receptor.
Bibliography:ObjectType-Article-1
SourceType-Scholarly Journals-1
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ISSN:0960-894X
1464-3405
DOI:10.1016/j.bmcl.2008.11.066