Identification of alpha-substituted acylamines as novel, potent, and orally active mGluR5 negative allosteric modulators
Bioorganic & Medicinal Chemistry Letters(2015)
Abstract
This Letter describes the identification of a series of novel non-acetylenic mGluR5 negative allosteric modulators based on the alpha-substituted acylamine structure. An initial structure–activity relationship study suggested that (R)-19b and (R)-19j might have good in vitro activity. When administered orally, these compounds were found to have an anxiolytic-like effect in a mouse model of stress-induced hyperthermia.
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Key words
Metabotropic glutamate receptor,mGluR5 negative allosteric modulators,Acylamines
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