Impact of the aryl substituent kind and distance from pyrimido[2,1-f]purindiones on the adenosine receptor selectivity and antagonistic properties

Adenosine receptor (AR) antagonists belong to two major groups of compounds: xanthines and non-xanthines. Recently several annelated xanthine derivatives have been described as selective A(1), A(2A), A(2B) and A(3) ARs antagonists. Contrary to dipropyl derivatives, in the group of dimethyl (un)substituted arylalkyl pyrimido[2,1-f]purindiones selective mainly adenosine A(2A) receptor antagonists were identified. Their activity depended on aryl substitution and its distance from pyrimido[2,1-f]purindione. (C) 2003 editions scientifiques et medicales Elsevier SAS. All rights reserved.