Biaryl and heteroaryl derivatives of SCH 58261 as potent and selective adenosine A 2A receptor antagonists

…, CD Boyle, S Chackalamannil, BR Neustadt…

Index: Shah, Unmesh; Boyle, Craig D.; Chackalamannil, Samuel; Neustadt, Bernard R.; Lindo, Neil; Greenlee, William J.; Foster, Carolyn; Arik, Leyla; Zhai, Ying; Ng, Kwokei; Wang, Shiyong; Monopoli, Angela; Lachowicz, Jean E. Bioorganic and Medicinal Chemistry Letters, 2008 , vol. 18, # 14 p. 4199 - 4203

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Citation Number: 14

Abstract

SCH 58261 is a reported adenosine A2A receptor antagonist, which is active in rat in vivo models of Parkinson's Disease upon ip administration. However, it has poor selectivity versus the A1 receptor and does not demonstrate oral activity. We report the design and synthesis of biaryl and heteroaryl analogs of SCH 58261 which improve the A2A receptor binding selectivity as well as the pharmacokinetic properties of SCH 58261. In particular, ...