title: Tricyclic heteroaromatic systems. Synthesis and benzodiazepine binding activity of 1-substituted-3-methyl- and 3-phenylpyrazolo[4,5-c]quinolin-4-ones.
abstract: The synthesis and the benzodiazepine binding activity of some 3-methyl- and 3-phenylpyrazolo[4,5-c]quinolin-4-ones bearing a heterocyclic or a substituent which is different from an aryl moiety at position-1 are reported. Molecular modelling is used to correlate the binding affinity to the chemical features and to justify the reduced receptor affinities of the reported compounds with respect to that of CGS 8216 which is taken as the lead compound.
authors.affiliation: Dipartimento di Scienze Farmaceutiche, Università di Firenze, Italy.
authors.forename: V
authors.initials: V
authors.lastname: Colotta
authors.forename: L
authors.initials: L
authors.lastname: Cecchi
authors.forename: F
authors.initials: F
authors.lastname: Melani
authors.forename: D
authors.initials: D
authors.lastname: Catarzi
authors.forename: G
authors.initials: G
authors.lastname: Filacchioni
authors.forename: C
authors.initials: C
authors.lastname: Martini
authors.forename: G
authors.initials: G
authors.lastname: Giannaccini
authors.forename: M
authors.initials: M
authors.lastname: Tonelli
authors.forename: A
authors.initials: A
authors.lastname: Lucacchini
mesh_terms: D000818:Animals; D002417:Cattle; D066298:In Vitro Techniques; D051379:Mice; D008958:Models, Molecular; D015363:Quinolones / Q000138:chemical synthesis* / Q000737:chemistry / Q000378:metabolism; D011963:Receptors, GABA-A / Q000378:metabolism*; D013329:Structure-Activity Relationship
chemical_list: D015363:Quinolones; D011963:Receptors, GABA-A