Abstract
New galanthamine derivatives, especially bis-interacting ligands 3-5 and 7-9 were prepared in order to interact with the catalytic and the peripheral sites of acetylcholinesterase (AChE). The synthesis, the anticholinesterase activities, and the structure-activity relationships of bis-interacting ligands are reported. Compounds 4d-e were found to be more potent than galanthamine and tacrine in inhibiting AChE.
Publication types
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Research Support, Non-U.S. Gov't
MeSH terms
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Acetylcholinesterase / drug effects*
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Acetylcholinesterase / metabolism
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Benzazepines / chemistry*
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Benzazepines / metabolism
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Benzazepines / pharmacology*
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Binding Sites
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Catalytic Domain
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Cholinesterase Inhibitors / chemistry*
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Cholinesterase Inhibitors / metabolism
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Cholinesterase Inhibitors / pharmacology*
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Drug Design
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Galantamine / chemistry*
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Phthalimides / chemistry*
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Phthalimides / metabolism
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Phthalimides / pharmacology*
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Structure-Activity Relationship
Substances
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9-dehydro-10-N-demethyl--10-N-(10'-phthalimidodecyl)galanthaminium
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9-dehydro-10-N-demethyl-10-N-(8'-phthalimidooctyl)galanthaminium
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Benzazepines
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Cholinesterase Inhibitors
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Phthalimides
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Galantamine
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Acetylcholinesterase