Peer-reviewed veterinary case report
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.
- Journal:
- Bioorganic & medicinal chemistry letters
- Year:
- 2005
- Authors:
- Matasi, Julius J et al.
- Affiliation:
- Department of Medicinal Chemistry-CV & CNS · United States
- Species:
- rodent
Abstract
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 A(2A) 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.
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Search related cases →Original publication: https://pubmed.ncbi.nlm.nih.gov/15978806/