Abstract
The complex etiology of Alzheimer's disease (AD) prompts scientists to develop multitarget strategies to combat causes and symptoms. We therefore designed, synthesized, and tested new hybrid molecules linking a benzofuran ring to a N-methyl- N-benzylamine through a heptyloxy chain, affording a series of potential multifunctional drugs for AD. The cholinesterase inhibitory activity was extended to the inhibition of Abeta fibril formation for 1, 3, and 5. Compound 3 showed an additional neuroprotective effect.
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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Amyloid / chemistry
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Amyloid / metabolism
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Amyloid beta-Peptides / chemistry*
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Amyloid beta-Peptides / metabolism
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Benzofurans / chemical synthesis*
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Benzofurans / chemistry
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Benzofurans / pharmacology
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Butyrylcholinesterase / chemistry
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Cell Line
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Cell Survival / drug effects
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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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Neurons / metabolism
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Peptide Fragments / chemistry*
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Peptide Fragments / metabolism
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Structure-Activity Relationship
Substances
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Amyloid
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Amyloid beta-Peptides
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Benzofurans
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Cholinesterase Inhibitors
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Peptide Fragments
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amyloid beta-protein (25-35)
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Acetylcholinesterase
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Butyrylcholinesterase