Potent and selective adenosine A 2A receptor antagonists: 1, 2, 4-Triazolo [1, 5-c] pyrimidines

…, S Fredduzzi, G Varty, M Cohen-Williams, K Ng

Index: Neustadt, Bernard R.; Liu, Hong; Hao, Jinsong; Greenlee, William J.; Stamford, Andrew W.; Foster, Carolyn; Arik, Leyla; Lachowicz, Jean; Zhang, Hongtao; Bertorelli, Rosalia; Fredduzzi, Silva; Varty, Geoffrey; Cohen-Williams, Mary; Ng, Kwokei Bioorganic and Medicinal Chemistry Letters, 2009 , vol. 19, # 3 p. 967 - 971

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Citation Number: 28

Abstract

Antagonism of the adenosine A2a receptor offers great promise in the treatment of Parkinson's disease. In the course of exploring pyrazolo [4, 3-e]-1, 2, 4-triazolo [1, 5-c] pyrimidine A2A antagonists, which led to clinical candidate SCH 420814, we prepared 1, 2, 4-triazolo [1, 5-c] pyrimidines with potent and selective (vs A1) A2a antagonist activity, including oral activity in the rat haloperidol-induced catalepsy model. Structure–activity ...