Discovery and biological profile of 4-(1-aryltriazol-4-yl)-tetrahydropyridines as an orally active new class of metabotropic glutamate receptor 1 antagonist.
Bioorg Med Chem
; 16(22): 9817-29, 2008 Nov 15.
Article
em En
| MEDLINE
| ID: mdl-18849168
ABSTRACT
We describe here the discovery and the structure-activity relationship (SAR) of a series of 4-(1-Aryltriazol-4-yl)-tetrahydropyridines as novel mGluR1 antagonists. Our extensive chemical modification of lead compound 2 successfully led to fluoropyridine analogs 7j and 1 with improved in vivo antagonistic activities. Among the evaluated compounds, chemically stable urea analog 1 showed oral antagonistic activity at dose ranges of 10-30mg/kg in an animal model.
Texto completo:
1
Base de dados:
MEDLINE
Assunto principal:
Piridinas
/
Receptores de Glutamato Metabotrópico
Idioma:
En
Ano de publicação:
2008
Tipo de documento:
Article