Abstract
Cage amines 1-4 are potent peripheral anionic site-bound reversible inhibitors of both acetylcholinesterase and butyrylcholinesterase. Cage amines 1-3 are selective butyrylcholinesterase inhibitor versus acetylcholinesterase. For both enzymes, the -log K(i) values linearly correlate with the difference of substituted phenyl radius of cage amines (-log K(i)=5.4+3.4Deltagamma for acetylcholinesterase, -log K(i)=5.9+3.2Deltagamma for butyrylcholinesterase). Moreover, the relationship between the enzymes and cage amines mimics that between bottles and stoppers.
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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Anions / chemistry
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Benzylamines / chemical synthesis
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Benzylamines / chemistry*
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Benzylamines / pharmacology*
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Binding Sites
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Butyrylcholinesterase / metabolism
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Cations / chemistry
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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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Edrophonium / pharmacology
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Electrophorus
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Horses
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Hydrolysis
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Kinetics
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Structure-Activity Relationship
Substances
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Anions
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Benzylamines
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Cations
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Cholinesterase Inhibitors
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Edrophonium
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Acetylcholinesterase
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Butyrylcholinesterase