Abstract
Imidazo[1,2-a]pyridines were identified via their shape and electrostatic similarity as novel positive allosteric modulators of the metabotropic glutamate 2 receptor. The subsequent synthesis and SAR are described. Potent, selective and metabolically stable compounds were found representing a promising avenue for current further studies.
Copyright 2009 Elsevier Ltd. All rights reserved.
MeSH terms
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Allosteric Regulation
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Animals
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Humans
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Imidazoles / chemistry*
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Microsomes, Liver / metabolism
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Pyridines / chemical synthesis
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Pyridines / chemistry*
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Pyridines / pharmacology
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Pyridones / chemistry*
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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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Static Electricity
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Structure-Activity Relationship
Substances
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Imidazoles
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Pyridines
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Pyridones
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Receptors, Metabotropic Glutamate
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metabotropic glutamate receptor 2
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imidazole