title: Design, synthesis, and preliminary pharmacological evaluation of 1, 4-diazabicyclo[4.3.0]nonan-9-ones as a new class of highly potent nootropic agents.
abstract: Several 4-substituted 1,4-diazabicyclo[4.3.0]nonan-9-ones have been synthesized and tested in vivo on mouse passive avoidance test, to evaluate their nootropic activity. The results show that they represent a new class of nootropic drugs with a pharmacological profile very similar to that of piracetam, showing much higher potency with respect to the reference. Among the compounds studied, 7 (DM 232) shows outstanding potency, being active at the dose of 0. 001 mg kg(-1) sc.
authors.affiliation: Dipartimento di Scienze Farmaceutiche, Università di Firenze, Via G. Capponi 9, I-50121 Firenze, Italy.
authors.forename: D
authors.initials: D
authors.lastname: Manetti
authors.forename: C
authors.initials: C
authors.lastname: Ghelardini
authors.forename: A
authors.initials: A
authors.lastname: Bartolini
authors.forename: C
authors.initials: C
authors.lastname: Bellucci
authors.forename: S
authors.initials: S
authors.lastname: Dei
authors.forename: N
authors.initials: N
authors.lastname: Galeotti
authors.forename: F
authors.initials: F
authors.lastname: Gualtieri
authors.forename: M N
authors.initials: MN
authors.lastname: Romanelli
authors.forename: S
authors.initials: S
authors.lastname: Scapecchi
authors.forename: E
authors.initials: E
authors.lastname: Teodori
mesh_terms: D000316:Adrenergic alpha-Agonists; D000647:Amnesia / Q000139:chemically induced / Q000188:drug therapy / Q000517:prevention & control; D000818:Animals; D001362:Avoidance Learning / Q000187:drug effects; D001418:Baclofen; D003000:Clonidine; D004305:Dose-Response Relationship, Drug; D015195:Drug Design; D018755:GABA Agonists; D008464:Mecamylamine; D051379:Mice; D015394:Molecular Structure; D018727:Muscarinic Antagonists; D009538:Nicotine / Q000037:antagonists & inhibitors; D018697:Nootropic Agents / Q000138:chemical synthesis* / Q000494:pharmacology*; D010879:Piperazines / Q000138:chemical synthesis* / Q000494:pharmacology* / Q000627:therapeutic use; D010889:Piracetam / Q000494:pharmacology; D011758:Pyrroles / Q000138:chemical synthesis* / Q000494:pharmacology* / Q000627:therapeutic use; D012601:Scopolamine
chemical_list: D000316:Adrenergic alpha-Agonists; D018755:GABA Agonists; D018727:Muscarinic Antagonists; D018697:Nootropic Agents; D010879:Piperazines; D011758:Pyrroles; D008464:Mecamylamine; D009538:Nicotine; D012601:Scopolamine; D001418:Baclofen; D003000:Clonidine; C409868:DM 232; D010889:Piracetam