Discovery of 2-aminoimidazopyridine adenosine A 2A receptor antagonists

BF McGuinness, AG Cole, G Dong, MR Brescia…

Index: McGuinness, Brian F.; Cole, Andrew G.; Dong, Guizhen; Brescia, Marc-Raleigh; Shao, Yuefei; Henderson, Ian; Rokosz, Laura L.; Stauffer, Tara M.; Mannava, Neelima; Kimble, Earl F.; Hicks, Catherine; White, Nicole; Wines, Pamela G.; Quadros, Elizabeth Bioorganic and Medicinal Chemistry Letters, 2010 , vol. 20, # 22 p. 6845 - 6849

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Citation Number: 8

Abstract

A novel series of adenosine A2A receptor antagonists was identified by high-throughput screening of an encoded combinatorial compound collection. The initial hits were optimized for A2A binding affinity, A1 selectivity, and in vitro microsomal stability generating orally available 2-aminoimidazo [4, 5-b] pyridine-based A2A antagonist leads.