3H-[1, 2, 4]-Triazolo [5, 1-i] purin-5-amine derivatives as adenosine A 2A antagonists

…, C Foster, R Bertorelli, A Monopoli, E Ongini

文献索引：Silverman, Lisa S.; Caldwell, John P.; Greenlee, William J.; Kiselgof, Eugenia; Matasi, Julius J.; Tulshian, Deen B.; Arik, Leyla; Foster, Carolyn; Bertorelli, Rosalia; Monopoli, Angela; Ongini, Ennio Bioorganic and Medicinal Chemistry Letters, 2007 , vol. 17, # 6 p. 1659 - 1662

全文：HTML全文

被引用次数: 18

摘要

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 ...