The discovery and synthesis of novel adenosine receptor (A 2A) antagonists

JJ Matasi, JP Caldwell, J Hao, B Neustadt, L Arik…

Index: Matasi, Julius J.; Caldwell, John P.; Hao, Jinsong; Neustadt, Bernard; Arik, Leyla; Foster, Carolyn J.; Lachowicz, Jean; Tulshian, Deen B. Bioorganic and Medicinal Chemistry Letters, 2005 , vol. 15, # 5 p. 1333 - 1336

Full Text: HTML

Citation Number: 45

Abstract

In high throughput screening of our file compounds, a novel structure 1 was identified as a potent A2A receptor antagonist with no selectivity over the A1 adenosine receptor. The structure–activity relationship investigation using 1 as a template lead to identification of a novel class of compounds as potent and selective antagonists of A2A adenosine receptor. Compound 26 was identified to be the most potent A2A receptor antagonist (Ki= 0.8 nM) ...