Discovery of biological evaluation of pyrazole/imidazole amides as mGlu5 receptor negative allosteric modulators.
Bioorg Med Chem Lett
; 23(7): 2134-9, 2013 Apr 01.
Article
em En
| MEDLINE
| ID: mdl-23434029
ABSTRACT
Development of SAR in a 5-aryl-3-acylpyridinyl-pyrazoles and 1-aryl-4-acylpyridinyl imidazoles series of mGlu5 receptor negative allosteric modulators (mGluR5 NAMs) using a functional cell-based assay is described in this Letter. Analysis of the Ligand-lipophilic efficiency (LipE) of compounds provided new insight for the design of potent mGluR5 negative allosteric modulators with anti-depressant activities.
Texto completo:
1
Coleções:
01-internacional
Base de dados:
MEDLINE
Assunto principal:
Pirazóis
/
Receptores de Glutamato Metabotrópico
/
Descoberta de Drogas
/
Amidas
/
Imidazóis
Limite:
Animals
/
Humans
Idioma:
En
Ano de publicação:
2013
Tipo de documento:
Article