Imidazo [2, 1-i] purin-5-ones and related tricyclic water-soluble purine derivatives: potent A2A-and A3-adenosine receptor antagonists

…, M Diekmann, KA Jacobson, WL Padgett…

Index: Mueller, Christa E.; Thorand, Mark; Qurishi, Ramatullah; Diekmann, Martina; Jacobson, Kenneth A.; Padgett, William L.; Daly, John W. Journal of Medicinal Chemistry, 2002 , vol. 45, # 16 p. 3440 - 3450

Full Text: HTML

Citation Number: 79

Abstract

A series of tricyclic imidazo [2, 1-i] purinones and ring-enlarged analogues derived from xanthine derivatives have been prepared as adenosine receptor (AR) antagonists. In comparison with xanthines, the tricyclic compounds exhibit increased water solubility due to a basic nitrogen atom, which can be protonated under physiological conditions. Substituents were introduced that confer high affinity for A2A or A3 ARs, respectively. A new capillary ...