title: Synthesis and pharmacological evaluation of pyrazolo[1,5-a]pyrimidin-7(4H)-one derivatives as potential GABAA-R ligands.
abstract: The synthesis of a new series of 6-phenyl- and 6-benzylpyrazolo[1,5-a]pyrimidin-7(4H)-ones 2a-g and 3a-g, strictly related to derivatives with pyrazolobenzotriazine (PBT) and pyrazoloquinazoline (PQ) scaffold, was realized. The in vitro GABAA-receptor subtype affinity was evaluated and from preliminary pharmacological studies, compound 3g shows anxiolytic-like effect at 10-30mg/kg.
authors.affiliation: Dipartimento NEUROFARBA, Sezione Farmaceutica e Nutraceutica, Università di Firenze, Via Ugo Schiff, 6 - 50019 Sesto Fiorentino, Firenze, Italy. Electronic address: gabriella.guerrini@unifi.it.
authors.forename: Gabriella
authors.initials: G
authors.lastname: Guerrini
authors.affiliation: Dipartimento NEUROFARBA, Sezione Farmaceutica e Nutraceutica, Università di Firenze, Via Ugo Schiff, 6 - 50019 Sesto Fiorentino, Firenze, Italy.
authors.forename: Giovanna
authors.initials: G
authors.lastname: Ciciani
authors.affiliation: Dipartimento di Farmacia, Università di Pisa, Via Bonanno 6, 56126 Pisa, Italy.
authors.forename: Simona
authors.initials: S
authors.lastname: Daniele
authors.affiliation: Dipartimento NEUROFARBA, Sezione Farmacologia e Tossicologia, Università di Firenze, Viale Gaetano Pieraccini, 6 - 50139 Firenze, Italy.
authors.forename: Lorenzo
authors.initials: L
authors.lastname: Di Cesare Mannelli
authors.affiliation: Dipartimento NEUROFARBA, Sezione Farmacologia e Tossicologia, Università di Firenze, Viale Gaetano Pieraccini, 6 - 50139 Firenze, Italy.
authors.forename: Carla
authors.initials: C
authors.lastname: Ghelardini
authors.affiliation: Dipartimento di Farmacia, Università di Pisa, Via Bonanno 6, 56126 Pisa, Italy.
authors.forename: Claudia
authors.initials: C
authors.lastname: Martini
authors.affiliation: Dipartimento NEUROFARBA, Sezione Farmaceutica e Nutraceutica, Università di Firenze, Via Ugo Schiff, 6 - 50019 Sesto Fiorentino, Firenze, Italy.
authors.forename: Silvia
authors.initials: S
authors.lastname: Selleri
mesh_terms: D000818:Animals; D014151:Anti-Anxiety Agents / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology; D002417:Cattle; D004305:Dose-Response Relationship, Drug; D008024:Ligands; D008297:Male; D051379:Mice; D011720:Pyrazoles / Q000737:chemistry*; D011743:Pyrimidines / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D051381:Rats; D017208:Rats, Wistar; D011963:Receptors, GABA-A / Q000378:metabolism*; D013329:Structure-Activity Relationship
chemical_list: D014151:Anti-Anxiety Agents; D008024:Ligands; D011720:Pyrazoles; D011743:Pyrimidines; D011963:Receptors, GABA-A
keywords: Drug design; GABA(A); Pyrazolo[1,5-a]pyrimidin-7(4H)one; Receptor