Oxadiazolone bioisosteres of pregabalin and gabapentin.
Bioorg Med Chem Lett
; 19(1): 247-50, 2009 Jan 01.
Article
em En
| MEDLINE
| ID: mdl-19010672
ABSTRACT
A series of oxadiazolone bioisosteres of pregabalin 1 and gabapentin 2 were prepared, and several were found to exhibit similar potency for the alpha(2)-delta subunit of voltage-gated calcium channels. Oxadiazolone 9 derived from 2 achieved low brain uptake but was nevertheless active in models of osteoarthritis. The high clearance associated with compound 9 was postulated to be a consequence of efflux by OAT and/or OCT, and was attenuated on co-administration with cimetidine or probenecid.
Texto completo:
1
Coleções:
01-internacional
Base de dados:
MEDLINE
Assunto principal:
Osteoartrite
/
Oxidiazóis
/
Ácidos Cicloexanocarboxílicos
/
Ácido gama-Aminobutírico
/
Aminas
Tipo de estudo:
Prognostic_studies
Limite:
Animals
Idioma:
En
Revista:
Bioorg Med Chem Lett
Ano de publicação:
2009
Tipo de documento:
Article