Norbornyllactone-substituted xanthines as adenosine A1 receptor antagonists Original Research Article

During the search for second-generation adenosine A1 receptor antagonist alternatives to the clinical candidate 8-(3-oxa-tricyclo[3.2.1.02,4]oct-6-yl)-1,3-dipropyl-3,7-dihydro-purine-2,6-dione (BG9719), we developed a series of novel xanthines substituted with norbornyl-lactones that possessed high binding affinities for adenosine A1 receptors and in vivo activity.