Abstract
Syntheses of certain di- and mono-oxygenated derivatives (e.g., 2 and 3, respectively) and analogues (e.g., 4, a D-ring monoseco-analogue of 2) of both the (-)- and (+)-enantiomeric forms of the alkaloid galanthamine [(-)-1] are reported. All have been assessed for their capacities to inhibit acetylcholine esterase but, in contrast to the predictions from docking studies, none bind strongly to this enzyme.
Publication types
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Research Support, Non-U.S. Gov't
MeSH terms
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Acetylcholinesterase / metabolism*
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Animals
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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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Dose-Response Relationship, Drug
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Electrophorus
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Galantamine / chemical synthesis
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Galantamine / chemistry
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Galantamine / pharmacology*
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Molecular Conformation
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Molecular Docking Simulation
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Stereoisomerism
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Structure-Activity Relationship
Substances
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Cholinesterase Inhibitors
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Galantamine
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Acetylcholinesterase