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 ,
Issue Information
روزنامه با شماره پیاپی سال 2007
Pages
4
From page
1659
To page
1662
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.
Keywords
Adenosine A2A receptor , Antagonist
Journal title
Bioorganic & Medicinal Chemistry Letters
Serial Year
2007
Journal title
Bioorganic & Medicinal Chemistry Letters
Record number
797907
Link To Document