1.
Bioorg Med Chem Lett
; 17(23): 6525-8, 2007 Dec 01.
Artículo
en Inglés
| MEDLINE
| ID: mdl-17936624
RESUMEN
We describe three novel regioisomeric series of aryl naphthyridine analogs, which are potent antagonists of the Class III GPCR mGlu5 receptor. The synthesis and in vitro and in vivo pharmacological activities of these analogs are discussed.
Asunto(s)
Naftiridinas/síntesis química , Naftiridinas/farmacología , Receptores de Glutamato Metabotrópico/antagonistas & inhibidores , Animales , Células CHO , Cricetinae , Cricetulus , Ratas , Receptor del Glutamato Metabotropico 5 , Receptores de Glutamato Metabotrópico/fisiología , Estereoisomerismo , Relación Estructura-Actividad
2.
Bioorg Med Chem Lett
; 17(16): 4415-8, 2007 Aug 15.
Artículo
en Inglés
| MEDLINE
| ID: mdl-17590335
RESUMEN
Rational replacement of the alkyne linker of mGluR5 antagonist MPEP gave 7-arylquinolines. SAR optimization gave an orally active compound with high affinity for the MPEP binding site.