1,1′-Xylyl bis-1,4,8,11-tetraaza cyclotetradecane: A new potential copper chelator agent for neuroprotection in Alzheimer’s disease. Its comparative effects with clioquinol on rat brain copper distribution

Dysfunction of copper metabolism leading to its excess or deficiency results in severe ailments. Recently, neurodegenerative disorders such as Alzheimer’s disease have been associated with copper metabolism. Compounds having the ability to reduce copper levels in brain or to affect its distribution...

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Bibliographic Details
Published in:Bioorganic & medicinal chemistry letters 2006-06, Vol.16 (12), p.3298-3301
Main Authors: Moret, Vincent, Laras, Younes, Pietrancosta, Nicolas, Garino, Cédrik, Quéléver, Gilles, Rolland, Amandine, Mallet, Bernard, Norreel, Jean-Chrétien, Kraus, Jean-Louis
Format: Article
Language:English
Subjects:
Alzheimer
Alzheimer Disease - cerebrospinal fluid
Alzheimer Disease - drug therapy
Alzheimer Disease - metabolism
Animals
Bicyclam
Biochemistry, Molecular Biology
Biological and medical sciences
Chelating Agents - pharmacokinetics
Chelating Agents - pharmacology
Clioquinol
Clioquinol - pharmacokinetics
Copper - metabolism
Copper brain distribution
Copper homeostasis
Heterocyclic Compounds, 1-Ring - chemistry
Heterocyclic Compounds, 1-Ring - pharmacology
Human health and pathology
Life Sciences
Medical sciences
Molecular Structure
Neuropharmacology
Neuroprotective agent
Pharmacology. Drug treatments
Psychoanaleptics: cns stimulant, antidepressant agent, nootropic agent, mood stabilizer..., (alzheimer disease)
Psychology. Psychoanalysis. Psychiatry
Psychopharmacology
Rats
Structure-Activity Relationship
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Summary:Dysfunction of copper metabolism leading to its excess or deficiency results in severe ailments. Recently, neurodegenerative disorders such as Alzheimer’s disease have been associated with copper metabolism. Compounds having the ability to reduce copper levels in brain or to affect its distribution could have neuroprotective effects, mainly through a downregulation of the transcription of amyloid peptide precursor (APP). We report here the biological effect of compound 1,1′-xylyl bis-1,4,8,11-tetraaza cyclotetradecane, which specifically affects copper concentration in the brain cortex region. Its copper homeostatic activity is compared with that of clioquinol, a well-known drug, which has been recently reported as an active Aβ-peptide clearance drug in vivo for Alzheimer’s patients.
ISSN:0960-894X
1464-3405
DOI:10.1016/j.bmcl.2006.03.026