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Peer-reviewed veterinary case report

Identification of alpha-substituted acylamines as novel, potent, and orally active mGluR5 negative allosteric modulators.

Journal:
Bioorganic & medicinal chemistry letters
Year:
2015
Authors:
Yoshikawa, Keita et al.
Affiliation:
Pharmaceutical Research Laboratories · Japan

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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Original publication: https://pubmed.ncbi.nlm.nih.gov/26112438/