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Evaluation of Homobivalent Carbolines as Designed Multiple Ligands for the Treatment of Neurodegenerative Disorders.
- Source :
-
Journal of medicinal chemistry [J Med Chem] 2015 Aug 27; Vol. 58 (16), pp. 6710-5. Date of Electronic Publication: 2015 Aug 17. - Publication Year :
- 2015
-
Abstract
- Neurodegenerative diseases represent a challenge for biomedical research due to their high prevalence and lack of mechanism-based treatments. Because of the complex pathology of neurodegenerative disorders, multifunctional drugs have been increasingly recognized as potential treatments. We identified homobivalent γ-carbolinium salts as potent inihitors of both cholinesterases, N-methyl-D-aspartate receptors, and monoamine oxidases. Homobivalent γ-carbolines displayed similar structure-activity relationships on all tested targets and may present promising designed multiple ligands for the treatment of neurodegenerative disorders.
- Subjects :
- Animals
Cholinesterase Inhibitors chemical synthesis
Cholinesterase Inhibitors pharmacology
Computational Biology
Excitatory Amino Acid Antagonists chemical synthesis
Excitatory Amino Acid Antagonists pharmacology
Humans
Indicators and Reagents
Ligands
Monoamine Oxidase Inhibitors chemical synthesis
Monoamine Oxidase Inhibitors pharmacology
Receptors, N-Methyl-D-Aspartate antagonists & inhibitors
Structure-Activity Relationship
Carbolines chemical synthesis
Carbolines therapeutic use
Neurodegenerative Diseases drug therapy
Subjects
Details
- Language :
- English
- ISSN :
- 1520-4804
- Volume :
- 58
- Issue :
- 16
- Database :
- MEDLINE
- Journal :
- Journal of medicinal chemistry
- Publication Type :
- Academic Journal
- Accession number :
- 26278660
- Full Text :
- https://doi.org/10.1021/acs.jmedchem.5b00958