Antagonists of the human A2A adenosine receptor. 4. Design, synthesis, and preclinical evaluation of 7-aryltriazolo [4, 5-d] pyrimidines

…, J Lerpiniere, S Leonardi, S Lightowler…

Index: Gillespie, Roger J.; Bamford, Samantha J.; Botting, Ruth; Comer, Mike; Denny, Sarah; Gaur, Suneel; Griffin, Michael; Jordan, Allan M.; Knight, Anthony R.; Lerpiniere, Joanne; Leonardi, Stefania; Lightowler, Sean; McAteer, Steven; Merrett, Angela; Misra, Anil; Padfield, Antony; Reece, Mark; Saadi, Mona; Selwood, Daniel L.; Stratton, Gemma C.; Surry, Dominic; Todd, Richard; Tong, Xin; Ruston, Vicki; Upton, Rebecca; Weiss, Scott M. Journal of Medicinal Chemistry, 2009 , vol. 52, # 1 p. 33 - 47

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Citation Number: 67

Abstract

Antagonism of the human A2A receptor has been implicated as a point of therapeutic intervention in the alleviation of the symptoms associated with Parkinson's disease. This is thought to occur, at least in part, by increasing the sensitivity of the dopaminergic neurons to the residual, depleted levels of striatal dopamine. We herein describe a novel series of functionalized triazolo [4, 5-d] pyrimidine derivatives that display functional antagonism of ...