Potent mGluR5 antagonists: pyridyl and thiazolyl-ethynyl-3,5-disubstituted-phenyl series.
Bioorg Med Chem Lett
; 21(11): 3243-7, 2011 Jun 01.
Article
em En
| MEDLINE
| ID: mdl-21546249
ABSTRACT
We report the synthesis of four series of 3,5-disubstituted-phenyl ligands targeting the metabotropic glutamate receptor subtype 5 (2-methylthiazol-4-yl)ethynyl (1a-j,), (6-methylpyridin-2-yl)ethynyl (2a-j), (5-methylpyridin-2-yl)ethynyl (3a-j,), and (pyridin-2-yl)ethynyl (4a-j,). The compounds were evaluated for antagonism of glutamate-mediated mobilization of internal calcium in an mGluR5 in vitro assay. All compounds were found to be full antagonists and exhibited low nanomolar to subnanomolar activity.
Texto completo:
1
Coleções:
01-internacional
Base de dados:
MEDLINE
Assunto principal:
Piridinas
/
Acetileno
/
Tiazóis
/
Receptores de Glutamato Metabotrópico
Limite:
Animals
Idioma:
En
Ano de publicação:
2011
Tipo de documento:
Article