Abstract
Cooperating mercapto groups with tacrine in a single molecular, novel multifunctional compounds have been designed and synthesized. These mercapto-tacrine derivatives displayed a synergistic pharmacological profile of long-term potentiation enhancement, cholinesterase inhibition, neuroprotection, and less hepatotoxicity, emerging as promising molecules for the therapy of age-related neurodegenerative diseases.
© 2012 American Chemical Society
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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Aging
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Animals
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Butyrylcholinesterase / chemistry
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CA1 Region, Hippocampal / drug effects
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CA1 Region, Hippocampal / physiology
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Cell Line, Tumor
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Cholinesterase Inhibitors / chemical synthesis*
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Cholinesterase Inhibitors / pharmacology
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Humans
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Liver / drug effects
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Long-Term Potentiation / drug effects
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Neurodegenerative Diseases / drug therapy*
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Neuroprotective Agents / chemical synthesis*
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Neuroprotective Agents / pharmacology
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Oxidative Stress / drug effects
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Rats
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Rats, Sprague-Dawley
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Structure-Activity Relationship
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Sulfhydryl Compounds / chemical synthesis*
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Sulfhydryl Compounds / pharmacology
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Tacrine / analogs & derivatives*
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Tacrine / chemical synthesis*
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Tacrine / pharmacology
Substances
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Cholinesterase Inhibitors
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Neuroprotective Agents
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Sulfhydryl Compounds
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Tacrine
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Acetylcholinesterase
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Butyrylcholinesterase