Octahydropyrrolo[3,4-c]pyrrole negative allosteric modulators of mGlu1.
Bioorg Med Chem Lett
; 23(18): 5091-6, 2013 Sep 15.
Article
em En
| MEDLINE
| ID: mdl-23932792
ABSTRACT
Development of SAR in an octahydropyrrolo[3,4-c]pyrrole series of negative allosteric modulators of mGlu1 using a functional cell-based assay is described in this Letter. The octahydropyrrolo[3,4-c]pyrrole scaffold was chosen as an isosteric replacement for the piperazine ring found in the initial hit compound. Characterization of selected compounds in protein binding assays was used to identify the most promising analogs, which were then profiled in P450 inhibition assays in order to further assess the potential for drug-likeness within this series of compounds.
Palavras-chave
Texto completo:
1
Base de dados:
MEDLINE
Assunto principal:
Pirróis
/
Receptores de Glutamato Metabotrópico
/
Inibidores Enzimáticos
Limite:
Animals
/
Humans
Idioma:
En
Ano de publicação:
2013
Tipo de documento:
Article