2-(2-furanyl)-7-(2-(4-(4-(2-methoxyethoxy)phenyl)-1-piperazinyl)ethyl)-7h-pyrazolo(4-3-e)(1-2-4)triazolo(1-5-c)pyrimidine-5-amine has been researched along with Parkinson-Disease* in 3 studies
3 other study(ies) available for 2-(2-furanyl)-7-(2-(4-(4-(2-methoxyethoxy)phenyl)-1-piperazinyl)ethyl)-7h-pyrazolo(4-3-e)(1-2-4)triazolo(1-5-c)pyrimidine-5-amine and Parkinson-Disease
| Article | Year |
|---|---|
Potent and selective adenosine A(2A) receptor antagonists: [1,2,4]-triazolo[4,3-c]pyrimidin-3-ones.
Antagonism of the adenosine A(2A) receptor affords a possible treatment of Parkinson's disease. In the course of investigating pyrazolo[4,3-e]-1,2,4-triazolo[1,5-c]pyrimidine A(2A) antagonists, we prepared [1,2,4]-triazolo[4,3-c]pyrimidin-3-ones with potent and selective (vs A(1)) A(2A) antagonist activity. Structure-activity relationships are described for this series. Topics: Adenosine A2 Receptor Antagonists; Humans; Parkinson Disease; Pyrimidinones; Receptor, Adenosine A2A; Structure-Activity Relationship | 2011 |
Potent and selective adenosine A2A receptor antagonists: 1,2,4-Triazolo[1,5-c]pyrimidines.
Antagonism of the adenosine A(2a) 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 A(2A) antagonists, which led to clinical candidate SCH 420814, we prepared 1,2,4-triazolo[1,5-c]pyrimidines with potent and selective (vs A(1)) A(2a) antagonist activity, including oral activity in the rat haloperidol-induced catalepsy model. Structure-activity relationships and plasma levels are described for this series. Topics: Adenosine A2 Receptor Antagonists; Administration, Oral; Animals; Area Under Curve; Catalepsy; Chemistry, Pharmaceutical; Drug Design; Haloperidol; Models, Chemical; Parkinson Disease; Pyrimidines; Rats; Structure-Activity Relationship; Triazoles | 2009 |
Potent, selective, and orally active adenosine A2A receptor antagonists: arylpiperazine derivatives of pyrazolo[4,3-e]-1,2,4-triazolo[1,5-c]pyrimidines.
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), which shows broad selectivity, good pharmacokinetic properties, and excellent in vivo activity. Topics: Adenosine A2 Receptor Antagonists; Administration, Oral; Animals; Catalepsy; Disease Models, Animal; Parkinson Disease; Piperazine; Piperazines; Pyrimidines; Rats; Structure-Activity Relationship; Substrate Specificity; Treatment Outcome | 2007 |