Title of article :
3H-[1,2,4]-Triazolo[5,1-i]purin-5-amine derivatives as adenosine A2A antagonists
Author/Authors :
Lisa S. Silverman، نويسنده , , John P. Caldwell، نويسنده , , William J. Greenlee، نويسنده , , Eugenia Kiselgof، نويسنده , , Julius J. Matasi، نويسنده , , Deen B. Tulshian، نويسنده , , Leyla Arik، نويسنده , , Carolyn Foster، نويسنده , , Rosalia Bertorelli، نويسنده , , Angela Monopoli، نويسنده , , Ennio Ongini، نويسنده ,
Abstract :
A novel series of 3-substituted-8-aryl-[1,2,4]-triazolo[5,1-i]purin-5-amine analogs related to Sch 58261 was synthesized in order to identify potent adenosine A2A receptor antagonists with improved selectivity over the A1 receptor, physiochemical properties, and pharmacokinetic profiles as compared to those of Sch 58261. As a result of structural modifications, numerous analogs with excellent in vitro binding affinities and selectivities were identified. Moreover, compound 27 displayed both superior in vitro and highly promising in vivo profiles.
