Abstract
Rational replacement of the alkyne linker of mGluR5 antagonist MPEP gave 7-arylquinolines. SAR optimization gave an orally active compound with high affinity for the MPEP binding site.
MeSH terms
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Drug Design*
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Excitatory Amino Acid Antagonists / chemistry*
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Excitatory Amino Acid Antagonists / pharmacology*
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Models, Molecular
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Molecular Structure
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Pyridines / chemistry
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Pyridines / pharmacology
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Quinolines / chemistry*
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Quinolines / pharmacology*
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Receptor, Metabotropic Glutamate 5
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Receptors, Metabotropic Glutamate / antagonists & inhibitors*
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Structure-Activity Relationship
Substances
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Excitatory Amino Acid Antagonists
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Pyridines
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Quinolines
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Receptor, Metabotropic Glutamate 5
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Receptors, Metabotropic Glutamate
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6-methyl-2-(phenylethynyl)pyridine