Phenyl isoxazole voltage-gated sodium channel blockers: structure and activity relationship.
Bioorg Med Chem Lett
; 21(13): 3871-6, 2011 Jul 01.
Article
em En
| MEDLINE
| ID: mdl-21641215
ABSTRACT
Blocking of certain sodium channels is considered to be an attractive mechanism to treat chronic pain conditions. Phenyl isoxazole carbamate 1 was identified as a potent and selective Na(V)1.7 blocker. Structural analogues of 1, both carbamates, ureas and amides, were proven to be useful in establishing the structure-activity relationship and improving ADME related properties. Amide 24 showed a good overall in vitro profile, that translated well to rat in vivo PK.
Texto completo:
1
Base de dados:
MEDLINE
Assunto principal:
Carbamatos
/
Bloqueadores dos Canais de Sódio
/
Isoxazóis
Limite:
Animals
/
Humans
Idioma:
En
Revista:
Bioorg Med Chem Lett
Assunto da revista:
BIOQUIMICA
/
QUIMICA
Ano de publicação:
2011
Tipo de documento:
Article
País de afiliação:
Suécia