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 an A(1) selectivity assay. Selected examples exhibited excellent affinity for A(2A) and good selectivity versus the A(1) receptor.
Cole
Andrew G
AG
Pharmacopeia, Inc., PO Box 5350, Princeton, NJ 08543, USA. acole@pcop.com
Stauffer
Tara M
TM
Rokosz
Laura L
LL
Metzger
Axel
A
Dillard
Lawrence W
LW
Zeng
Wenguang
W
Henderson
Ian
I
D000478:Alkylation; D002460:Cell Line; D020650:Combinatorial Chemistry Techniques; D055808:Drug Discovery; D006801:Humans; D058915:Purinergic P1 Receptor Antagonists; D011869:Radioligand Assay; D018047:Receptors, Purinergic P1 / Q000378:metabolism; D013844:Thiazoles / Q000138:chemical synthesis* / Q000378:metabolism / Q000494:pharmacology*
D058915:Purinergic P1 Receptor Antagonists; D018047:Receptors, Purinergic P1; D013844:Thiazoles