Antagonists of the human adenosine A 2A receptor. Part 1: discovery and synthesis of thieno [3, 2-d] pyrimidine-4-methanone derivatives

…, D Bebbington, K Benwell, IA Cliffe, CE Dawson…

Index: Gillespie, Roger J.; Adams, David R.; Bebbington, David; Benwell, Karen; Cliffe, Ian A.; Dawson, Claire E.; Dourish, Colin T.; Fletcher, Allan; Gaur, Suneel; Giles, Paul R.; Jordan, Allan M.; Knight, Antony R.; Knutsen, Lars J.S.; Lawrence, Anthony; Lerpiniere, Joanne; Misra, Anil; Porter, Richard H.P.; Pratt, Robert M.; Shepherd, Robin; Upton, Rebecca; Ward, Simon E.; Weiss, Scott M.; Williamson, Douglas S. Bioorganic and Medicinal Chemistry Letters, 2008 , vol. 18, # 9 p. 2916 - 2919

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Citation Number: 36

Abstract

The (−)-(11R, 2′ S)-enantiomer of the antimalarial drug mefloquine has been found to be a reasonably potent and moderately selective adenosine A2A receptor antagonist. Further investigation of this compound has led to the discovery of a series of keto-aryl thieno [3, 2-d] pyrimidine derivatives, which are potent and selective antagonists of the adenosine A2A receptor. These derivatives show selectivity against the A1 receptor. Furthermore, some of ...