Abstract
The coupling of two different pharmacophores, each endowed with different biological properties, afforded the hybrid compound lipocrine (7), whose biological profile was markedly improved relative to those of prototypes tacrine and lipoic acid. Lipocrine is the first compound that inhibits the catalytic activity of AChE and AChE-induced amyloid-beta aggregation and protects against reactive oxygen species. Thus, it emerged as a valuable pharmacological tool to investigate Alzheimer's disease and as a promising lead compound for new anti-Alzheimer drugs.
Publication types
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Research Support, Non-U.S. Gov't
MeSH terms
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Acetylcholinesterase / chemistry
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Alzheimer Disease / drug therapy
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Amyloid beta-Peptides / chemistry
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Antioxidants / chemical synthesis*
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Antioxidants / chemistry
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Antioxidants / pharmacology
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Butyrylcholinesterase / chemistry
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Cell Line
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Cholinesterase Inhibitors / chemical synthesis*
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Cholinesterase Inhibitors / chemistry
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Cholinesterase Inhibitors / pharmacology
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Humans
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Neurons / cytology
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Neurons / drug effects
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Nootropic Agents / chemical synthesis*
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Nootropic Agents / chemistry
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Nootropic Agents / pharmacology
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Reactive Oxygen Species / metabolism
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Structure-Activity Relationship
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Tacrine / analogs & derivatives*
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Tacrine / chemical synthesis*
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Tacrine / chemistry
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Tacrine / pharmacology
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Thioctic Acid / analogs & derivatives*
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Thioctic Acid / chemical synthesis*
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Thioctic Acid / chemistry
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Thioctic Acid / pharmacology
Substances
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Amyloid beta-Peptides
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Antioxidants
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Cholinesterase Inhibitors
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Nootropic Agents
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Reactive Oxygen Species
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lipocrine
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Tacrine
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Thioctic Acid
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Acetylcholinesterase
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Butyrylcholinesterase