Synthesis and A1-adenosine receptors affinities of purino[7,8-c]quinazoline-8,10(9H,11H)-diones as rigid analogues of 8-arylxanthines

Title compounds were prepared by a cyclocondensation reaction between 8-(2-aminophenyl)xanthines and trialkyl orthoesters. Some of them showed activities as A1-adenosine receptor antagonists with binding values in the micromolar range. Results are discussed with reference to 1,3-dialkyl-8-arylxanthi...

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Bibliographic Details
Published in:	Farmaco (Società chimica italiana : 1989) Vol. 48; no. 9; p. 1301
Main Authors:	Ceccarelli, S, D'Alessandro, A, Magnante, F, Scuri, R, Zanarella, S
Format:	Journal Article
Language:	English
Published:	France 01-09-1993
Subjects:	Animals Cerebral Cortex - metabolism In Vitro Techniques Quinazolines - chemical synthesis Quinazolines - metabolism Rats Receptors, Purinergic P1 - metabolism
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Summary:	Title compounds were prepared by a cyclocondensation reaction between 8-(2-aminophenyl)xanthines and trialkyl orthoesters. Some of them showed 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 electronic and conformational factors are also reported.
ISSN:	0014-827X