Propidium-Based Polyamine Ligands as Potent Inhibitors of Acetylcholinesterase and Acetylcholinesterase-Induced Amyloid-β Aggregation

Heterodimers 4 and 5 were effective inhibitors of acetylcholinesterase (AChE) activity and AChE-induced amyloid-β (Aβ) aggregation. The peculiar biological profile of 4 can be relevant in studying the molecular basis underlying the nonclassical action of AChE and in addressing the question whether A...

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Bibliographic Details
Published in:Journal of medicinal chemistry 2005-01, Vol.48 (1), p.24-27
Main Authors: Bolognesi, Maria Laura, Andrisano, Vincenza, Bartolini, Manuela, Banzi, Rita, Melchiorre, Carlo
Format: Article
Language:English
Subjects:
Acetylcholinesterase - drug effects
Acetylcholinesterase - metabolism
Amyloid beta-Peptides - drug effects
Amyloid beta-Peptides - metabolism
Biochemistry - methods
Biological and medical sciences
Cholinesterase Inhibitors - chemistry
Cholinesterase Inhibitors - metabolism
Cholinesterase Inhibitors - pharmacology
Dimerization
Drug Design
Drug Evaluation, Preclinical - methods
Fluorometry - methods
Humans
Hydrolysis
Inhibitory Concentration 50
Ligands
Medical sciences
Neuropharmacology
Pharmacology. Drug treatments
Polyamines - chemistry
Propidium - chemistry
Psychoanaleptics: cns stimulant, antidepressant agent, nootropic agent, mood stabilizer..., (alzheimer disease)
Psychology. Psychoanalysis. Psychiatry
Psychopharmacology
Structure-Activity Relationship
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Description
Summary:Heterodimers 4 and 5 were effective inhibitors of acetylcholinesterase (AChE) activity and AChE-induced amyloid-β (Aβ) aggregation. The peculiar biological profile of 4 can be relevant in studying the molecular basis underlying the nonclassical action of AChE and in addressing the question whether AChE inhibitors can affect the neurotoxic cascade leading to Alzheimer's disease. Compound 4 emerged as the most potent heterodimer so far available to inhibit AChE-induced Aβ aggregation.
ISSN:0022-2623
1520-4804
DOI:10.1021/jm049156q