Molecular simplification of 1,4-diazabicyclo[4.3.0]nonan-9-ones gives piperazine derivatives that maintain high nootropic activity

Journal of Medicinal Chemistry

Volumn 43, Issue 23, 2000, Pages 4499-4507

  Manetti, D ^a   Ghelardini, C ^a   Bartolini, A ^a   Dei, S ^a   Galeotti, N ^a   Gualtieri, F ^a   Romanelli, M N ^a   Teodori, E ^a  

^a UNIVERSITY OF FLORENCE   (Italy)

Author keywords

[No Author keywords available]

Indexed keywords

1,4 DIAZABICYCLO[4.3.0]NONAN 9 ONE; 2 PYRROLIDINONE; FR 121196; N (4 ACETYL 1 PIPERAZINYL) 4 FLUOROBENZAMIDE; N (4 ACETYL 1 PIPERAZINYL) 4 FLUOROBENZENESULFONAMIDE; NOOTROPIC AGENT; PIPERAZINE DERIVATIVE; UNCLASSIFIED DRUG;

ACETYLCHOLINE RELEASE; ARTICLE; DRUG ACTIVITY; DRUG POTENCY; PASSIVE AVOIDANCE; STRUCTURE ACTIVITY RELATION; SYNTHESIS;

ACETYLCHOLINE; ANALGESICS; ANIMALS; AVOIDANCE LEARNING; BICYCLO COMPOUNDS, HETEROCYCLIC; MALE; MEMORY; MICE; MICRODIALYSIS; NOOTROPIC AGENTS; PARIETAL LOBE; PIPERAZINES; RATS; RATS, WISTAR; SOCIAL BEHAVIOR; STRUCTURE-ACTIVITY RELATIONSHIP;

EID: 0034676320     PISSN: 00222623     EISSN: None     Source Type: Journal    
DOI: 10.1021/jm000972h     Document Type: Article

References (27)

1. Piracetam and other structurally related nootropics
2. In search of the mechanism of action of the nootropics: New insights potential clinical implications
3. Piracetam: Novelty in a unique mode of action
4. Psychostimulants, analeptics, nootropics: An attempt to differentiate assess drugs designed for the treatment of impaired brain functions
5. Cognitive enhancement therapy for Alzheimer's disease
6. Long-term and high-dose piracetam treatment of Alzheimer's disease
7. Design, synthesis and preliminary pharmacological evaluation of 1,4-diazabicyclo[4.3.0]nonan-9-ones as a new class of highly potent nootropic drugs
8. FK 960 [N-(4-acetyl-1-piperazinyl)p-fluorobenzamide monohydrate], a novel potential antidementia drug, improves visual recognition memory in rhesus monkeys: Comparison with physostigmine
9. Effect of FR121196, a novel cognitive enhancer, on the memory impairment of rats in passive avoidance and radial arm maze tasks
10. Preparation of anellated α-(piperazinylalkyl)indoles and related compounds as drugs. Kali-Chemie pharma GmbH, Ger. Offen. DE 4,128,015 1993
11. Preparation of mono-N-alkyl- and -N-acyl piperazines by non-hydrolytic cleavage of 1-carbethoxypiperazines
12. 7-(3-(1-piperidinyl)propoxy)chromenones as potential atypical antipsychotics
13. 4-substituents and its influence on the pharmacological activity in 2-methylpiperazine derivatives
14. An improved one-trial passive avoidance learning situation
15. B receptor blocker improves the cognitive performance of mice, rats and rhesus monkeys
16. Effect of thyrotropin releasing hormone (TRH) on acetylcholine release from different brain areas investigated by microdialysis
17. Quantification of the analgesic activity of narcotic antagonists by a modified hot-plate procedure
18. Chiral synthesis and pharmacological evaluation of the enantiomers of SM32, a new analgesic and cognition-enhancing agent
19. The frozen analogue approach in medicinal chemistry
20. The cholinergic hypothesis of geriatric memory dysfunctions
21. Nootropic drugs and brain cholinergic mechanisms
22. The medicinal chemistry of Alzheimer and Alzheimer-like diseases with emphasis on the cholinergic hypothesis
23. 3-α-Tropanyl 2-(4-Cl-phenoxy)butyrate (SM21): A review of the pharmacological profile of a novel enhancer of cholinergic transmission
24. Role of somastatin in the augmentation of hippocampal long-term potentiation by FR121196, a putative cognition enhancer
25. Synthesis of 1,4-substituted-2-methylpiperazines and study of their analgesic properties
26. Determination of acetylcholine in the femtomole range by means of HPLC, a postcolumn enzyme reactor, and electrochemical detection