- Potent and selective adenosine A2A receptor antagonists: 1,2,4-Triazolo[1,5-c]pyrimidines
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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 relationships and plasma levels are described for this series.
- 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
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scheme or table
p. 967 - 971
(2009/09/06)
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- 2-(2-Furanyl)-7-phenyl[1,2,4]triazolo[1,5-c]pyrimidin-5-amine analogs: Highly potent, orally active, adenosine A2A antagonists. Part 1
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The structure-activity relationship of this novel class of compounds based on 2-(2-furanyl)-7-phenyl[1,2,4]-triazolo[1,5-c]pyrimidin-5-amine, 1, and its analogs was evaluated for their in vitro and in vivo adenosine A2A receptor antagonism. Several compounds displayed oral activity at 3 mg/kg in a rat catalepsy model. Specifically, compound 8g displayed an excellent in vitro profile, as well as a highly promising in vivo profile.
- Matasi, Julius J.,Caldwell, John P.,Zhang, Hongtao,Fawzi, Ahmad,Cohen-Williams, Mary E.,Varty, Geoffrey B.,Tulshian, Deen B.
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p. 3670 - 3674
(2007/10/03)
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