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.
MeSH terms
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Animals
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Carbolines / chemical synthesis*
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Carbolines / therapeutic use*
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Cholinesterase Inhibitors / chemical synthesis
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Cholinesterase Inhibitors / pharmacology
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Computational Biology
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Excitatory Amino Acid Antagonists / chemical synthesis
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Excitatory Amino Acid Antagonists / pharmacology
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Humans
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Indicators and Reagents
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Ligands
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Monoamine Oxidase Inhibitors / chemical synthesis
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Monoamine Oxidase Inhibitors / pharmacology
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Neurodegenerative Diseases / drug therapy*
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Receptors, N-Methyl-D-Aspartate / antagonists & inhibitors
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Structure-Activity Relationship
Substances
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Carbolines
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Cholinesterase Inhibitors
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Excitatory Amino Acid Antagonists
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Indicators and Reagents
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Ligands
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Monoamine Oxidase Inhibitors
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Receptors, N-Methyl-D-Aspartate