S. Ceccarelli et al., SYNTHESIS AND A(1)-ADENOSINE RECEPTORS AFFINITIES OF PURINO[7,8-C]QUINAZOLINE-8,10(9H,11H)-DIONES AS RIGID ANALOGS OF 8-ARYLXANTHINES, Il Farmaco, 48(9), 1993, pp. 1301-1312
Title compounds were prepared by a cyclocondensation reaction between
8-(2-aminophenyl)xanthines and trialkyl orthoesters. Some of them show
ed activities as A1-adenosine receptor antagonists with binding values
in the micromolar range. Results are discussed with reference to 1,3-
dialkyl-8-arylxanthines. Considerations on the role played by both ele
ctronic and conformational factors are also reported.