Potent, selective, and orally active adenosine A 2A receptor antagonists: arylpiperazine derivatives of pyrazolo [4, 3-e]-1, 2, 4-triazolo [1, 5-c] pyrimidines

…, R Bertorelli, C Foster, L Arik, J Lachowicz, K Ng…

Index: Neustadt, Bernard R.; Hao, Jinsong; Lindo, Neil; Greenlee, William J.; Stamford, Andrew W.; Tulshian, Deen; Ongini, Ennio; Hunter, John; Monopoli, Angela; Bertorelli, Rosalia; Foster, Carolyn; Arik, Leyla; Lachowicz, Jean; Ng, Kwokei; Feng, Kung-I Bioorganic and Medicinal Chemistry Letters, 2007 , vol. 17, # 5 p. 1376 - 1380

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Citation Number: 105

Abstract

Antagonism of the adenosine A2A receptor offers great promise in the treatment of Parkinson's disease. Employing the known pyrazolo [4, 3-e]-1, 2, 4-triazolo [1, 5-c] pyrimidine A2A antagonist SCH 58261 as a starting point, we identified the potent and selective (vs. A1) antagonist 11h, orally active in the rat haloperidol-induced catalepsy model. We further optimized this lead to the methoxyethoxyethyl ether 12a (SCH 420814), ...