Abstract
We synthesized a series of N(1)-substituted norcymserine derivatives 7a-p and evaluated their anti-cholinesterase activities. In vitro evaluation showed that the pyridinylethyl derivatives 7m-o and the piperidinylethyl derivative 7p improved the anti-butyrylcholinesterase activity by approximately threefold compared to N(1)-phenethylnorcymserine (PEC, 2). A quantitative structure-activity relationship (QSAR) study indicated that logS might be a key feature of the improved compounds.
Copyright 2010 Elsevier Ltd. All rights reserved.
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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Acetylcholinesterase / metabolism
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Butyrylcholinesterase / chemistry*
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Butyrylcholinesterase / metabolism
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Carbamates / chemical synthesis*
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Carbamates / chemistry
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Carbamates / pharmacology
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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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Drug Design
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Humans
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Neuroprotective Agents / chemical synthesis*
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Neuroprotective Agents / chemistry
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Neuroprotective Agents / pharmacology
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Physostigmine / analogs & derivatives*
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Physostigmine / chemistry
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Quantitative Structure-Activity Relationship
Substances
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Carbamates
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Cholinesterase Inhibitors
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Neuroprotective Agents
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Physostigmine
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Acetylcholinesterase
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Butyrylcholinesterase