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

…, A Metzger, LW Dillard, W Zeng, I Henderson

文献索引：Cole, Andrew G.; Stauffer, Tara M.; Rokosz, Laura L.; Metzger, Axel; Dillard, Lawrence W.; Zeng, Wenguang; Henderson, Ian Bioorganic and Medicinal Chemistry Letters, 2009 , vol. 19, # 2 p. 378 - 381

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被引用次数: 23

摘要

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.