1.
Bioorg Med Chem Lett
; 25(16): 3135-41, 2015 Aug 15.
Artigo
em Inglês
| MEDLINE
| ID: mdl-26112438
RESUMO
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.