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

Pharmacopeia, Inc., PO Box 5350, Princeton, NJ 08543, USA.
Bioorganic & medicinal chemistry letters (Impact Factor: 2.33). 12/2008; 19(2):378-81. DOI: 10.1016/j.bmcl.2008.11.066
Source: PubMed

ABSTRACT 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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