Potent and selective adenosine A2A receptor antagonists: 1,2,4-Triazolo[1,5-c]pyrimidines |
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| Authors: | Bernard R Neustadt Hong Liu Jinsong Hao William J Greenlee Andrew W Stamford Carolyn Foster Leyla Arik Jean Lachowicz Hongtao Zhang Rosalia Bertorelli Silva Fredduzzi Geoffrey Varty Mary Cohen-Williams Kwokei Ng |
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| Institution: | 1. Departments of Chemical Research, CNS Pharmacology, Drug Metabolism and Pharmacokinetics, Schering-Plough Research Institute, 2015 Galloping Hill Road, Kenilworth, NJ 07033-1310, USA;2. Schering-Plough Research Institute, San Raffaele Science Park, 20132 Milan, Italy |
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| Abstract: | Antagonism of the adenosine A2a receptor offers great promise in the treatment of Parkinson’s disease. In the course of exploring pyrazolo4,3-e]-1,2,4-triazolo1,5-c]pyrimidine A2A antagonists, which led to clinical candidate SCH 420814, we prepared 1,2,4-triazolo1,5-c]pyrimidines with potent and selective (vs A1) A2a antagonist activity, including oral activity in the rat haloperidol-induced catalepsy model. Structure–activity relationships and plasma levels are described for this series. |
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