title: Synthesis and A1-adenosine receptors affinities of purino[7,8-c]quinazoline-8,10(9H,11H)-diones as rigid analogues of 8-arylxanthines.
abstract: 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.
authors.affiliation: Centro Ricerche del Consorzio Biomedica Foscama-Irfi, Ferentino, Italia.
authors.forename: S
authors.initials: S
authors.lastname: Ceccarelli
authors.forename: A
authors.initials: A
authors.lastname: D'Alessandro
authors.forename: F
authors.initials: F
authors.lastname: Magnante
authors.forename: R
authors.initials: R
authors.lastname: Scuri
authors.forename: S
authors.initials: S
authors.lastname: Zanarella
mesh_terms: D000818:Animals; D002540:Cerebral Cortex / Q000378:metabolism; D066298:In Vitro Techniques; D011799:Quinazolines / Q000138:chemical synthesis* / Q000378:metabolism*; D051381:Rats; D018047:Receptors, Purinergic P1 / Q000378:metabolism*
chemical_list: D011799:Quinazolines; D018047:Receptors, Purinergic P1