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.
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.
Manetti
D
D
Dipartimento di Scienze Farmaceutiche, Università di Firenze, Via G. Capponi 9, I-50121 Firenze, Italy.
Ghelardini
C
C
Bartolini
A
A
Bellucci
C
C
Dei
S
S
Galeotti
N
N
Gualtieri
F
F
Romanelli
M N
MN
Scapecchi
S
S
Teodori
E
E
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
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