Article ID | Journal | Published Year | Pages | File Type |
---|---|---|---|---|
1378561 | Bioorganic & Medicinal Chemistry Letters | 2005 | 5 Pages |
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.
Graphical abstractThe 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. Compound 8g displayed an excellent in vitro profile as well as a highly promising in vivo profile.Figure optionsDownload full-size imageDownload as PowerPoint slide