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Preparation of Cyclo‐Phen‐Type Ligands: Chelators of Metal Ions as Potential Therapeutic Agents in the Treatment of Neurodegenerative Diseases
Author(s) -
Boldron Christophe,
Van der Auwera Ingrid,
Deraeve Céline,
Gornitzka Heinz,
Wera Stefaan,
Pitié Marguerite,
Van Leuven Fred,
Meunier Bernard
Publication year - 2005
Publication title -
chembiochem
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 1.05
H-Index - 126
eISSN - 1439-7633
pISSN - 1439-4227
DOI - 10.1002/cbic.200500220
Subject(s) - chelation , chemistry , in vivo , thioflavin , zinc , ligand (biochemistry) , clioquinol , amyloid (mycology) , combinatorial chemistry , pharmacology , genetically modified mouse , derivative (finance) , stereochemistry , transgene , biochemistry , alzheimer's disease , receptor , disease , medicine , biology , organic chemistry , inorganic chemistry , pathology , microbiology and biotechnology , gene , financial economics , economics
A promising strategy for the therapy of neurodegenerative diseases consists of the use of chelators. A new cyclic derivative, Cyclo‐bi‐Phen, was synthesized in one step and found to complex copper and zinc. When used in i.p. injection at 5 mg kg −1 three times per week on double‐transgenic mice, this Cyclo‐bi‐Phen ligand (shown) was able to reduce in vivo Thioflavin‐S‐stainable amyloid plaques involved in the deleterious effects of the Alzheimer's disease.