title: Tricyclic heteroaromatic systems 1,2,4-triazolo[1,5-a]quinoxalines: synthesis and benzodiazepine receptor activity.
abstract: The synthesis, the benzodiazepine binding activity and the "in vitro" biological effect of some 1,2,4-triazolo[1,5-a]quinoxalines, 3-aza-analogues of some previously reported pyrazolo[1,5-a]quinoxalines, are described. Molecular modelling is used to define the structural requirements of the benzodiazepine recognition site which influence the affinity and different efficacy of these rigid ligands.
authors.affiliation: Dipartimento di Scienze Farmaceutiche, Università di Firenze, Italy.
authors.forename: D
authors.initials: D
authors.lastname: Catarzi
authors.forename: L
authors.initials: L
authors.lastname: Cecchi
authors.forename: V
authors.initials: V
authors.lastname: Colotta
authors.forename: F
authors.initials: F
authors.lastname: Melani
authors.forename: G
authors.initials: G
authors.lastname: Filacchioni
authors.forename: C
authors.initials: C
authors.lastname: Martini
authors.forename: L
authors.initials: L
authors.lastname: Giusti
authors.forename: A
authors.initials: A
authors.lastname: Lucacchini
mesh_terms: D000818:Animals; D001667:Binding, Competitive / Q000187:drug effects; D002417:Cattle; D002540:Cerebral Cortex / Q000187:drug effects / Q000378:metabolism; D002707:Chlordiazepoxide / Q000494:pharmacology; D005445:Flunitrazepam / Q000493:pharmacokinetics; D066298:In Vitro Techniques; D011810:Quinoxalines / Q000138:chemical synthesis* / Q000494:pharmacology; D011963:Receptors, GABA-A / Q000187:drug effects* / Q000378:metabolism; D014230:Triazoles / Q000138:chemical synthesis* / Q000494:pharmacology
chemical_list: D011810:Quinoxalines; D011963:Receptors, GABA-A; D014230:Triazoles; D005445:Flunitrazepam; D002707:Chlordiazepoxide