GluK1 antagonists from 6-(carboxy)phenyl decahydroisoquinoline derivatives. SAR and evaluation of a prodrug strategy for oral efficacy in pain models.
Bioorg Med Chem Lett
; 23(23): 6459-62, 2013 Dec 01.
Article
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| MEDLINE
| ID: mdl-24119554
ABSTRACT
The synthesis and structure-activity relationship of decahydroisoquinoline derivatives with various benzoic acid substitutions as GluK1 antagonists are described. Potent and selective antagonists were selected for a tailored prodrug approach in order to facilitate the evaluation of the new compounds in pain models after oral administration. Several diester prodrugs allowed for acceptable amino acid exposure and moderate efficacy in vivo.
Palabras clave
Texto completo:
1
Bases de datos:
MEDLINE
Asunto principal:
Dolor
/
Profármacos
/
Receptores de Ácido Kaínico
/
Isoquinolinas
Límite:
Animals
Idioma:
En
Revista:
Bioorg Med Chem Lett
Asunto de la revista:
BIOQUIMICA
/
QUIMICA
Año:
2013
Tipo del documento:
Article