Abstract
This Letter describes the synthesis and SAR of the novel positive allosteric modulator, VU0155041, a compound that has shown in vivo efficacy in rodent models of Parkinson's disease. The synthesis takes advantage of an iterative parallel synthesis approach to rapidly synthesize and evaluate a number of analogs of VU0155041.
Publication types
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Research Support, N.I.H., Extramural
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Research Support, Non-U.S. Gov't
MeSH terms
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Allosteric Regulation / drug effects
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Allosteric Site
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Anilides / chemical synthesis*
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Anilides / chemistry
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Anilides / pharmacology
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Animals
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Cyclohexanecarboxylic Acids / chemical synthesis*
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Cyclohexanecarboxylic Acids / chemistry
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Cyclohexanecarboxylic Acids / pharmacology
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Disease Models, Animal
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Parkinson Disease / drug therapy
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Rats
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Receptors, Metabotropic Glutamate / chemistry*
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Receptors, Metabotropic Glutamate / metabolism
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Structure-Activity Relationship
Substances
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Anilides
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Cyclohexanecarboxylic Acids
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Receptors, Metabotropic Glutamate
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VU 0155041
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metabotropic glutamate receptor 4