title: 1,2,3-triazolo[1.5-a]quinazolines: synthesis, benzodiazepine receptor binding and theoretical calculations.
abstract: This paper reports the synthesis of 3-substituted-1,2,3-triazolo[1,5-a]quinazolin-5-ones prepared by 1,3-dipolar cycloaddition reaction of 2-azidobenzoic acid to methylenic compounds activated by a cyano group. The new derivatives were submitted to benzodiazepine receptor binding assays: the results indicated an interesting receptorial affinity of the 1,2,3-triazolo[1,5-a]quinazoline ring. On the basis of the biological results, theoretical calculations were performed, which suggested useful structural modifications.
authors.affiliation: Dipartimento di Scienze Farmaceutiche, Facolta di Farmacia, Universita di Pisa, Italy.
authors.forename: G
authors.initials: G
authors.lastname: Biagi
authors.forename: I
authors.initials: I
authors.lastname: Giorgi
authors.forename: O
authors.initials: O
authors.lastname: Livi
authors.forename: V
authors.initials: V
authors.lastname: Scartoni
authors.forename: S
authors.initials: S
authors.lastname: Velo
authors.forename: A
authors.initials: A
authors.lastname: Lucacchini
authors.forename: G
authors.initials: G
authors.lastname: Senatore
authors.forename: B
authors.initials: B
authors.lastname: De Santis
authors.forename: A
authors.initials: A
authors.lastname: Martinelli
mesh_terms: D000818:Animals; D002417:Cattle; D005442:Flumazenil / Q000378:metabolism; D011799:Quinazolines / Q000138:chemical synthesis* / Q000378:metabolism / Q000494:pharmacology; D011963:Receptors, GABA-A / Q000187:drug effects* / Q000378:metabolism; D013329:Structure-Activity Relationship
chemical_list: D011799:Quinazolines; D011963:Receptors, GABA-A; D005442:Flumazenil