Structure-activity studies of a novel series of isoxazole-3-carboxamide derivatives as TRPV1 antagonists.
Bioorg Med Chem Lett
; 21(3): 892-8, 2011 Feb 01.
Article
em En
| MEDLINE
| ID: mdl-21236666
ABSTRACT
Optimisation of a screening hit incorporating both TRPV1 activity and solubility was conducted. Substitution of the isoxazole-3-carboxamide with the bespoke 1S, 3R-3-aminocyclohexanol motif afforded the requisite balance of potency and solubility. Compounds 32 and 40 were found to have antihyperalgesic effects in the rat CFA Hg assay and induce a mechanism based hyperthermia.
Texto completo:
1
Coleções:
01-internacional
Base de dados:
MEDLINE
Assunto principal:
Cicloexanóis
/
Canais de Cátion TRPV
/
Amidas
/
Isoxazóis
/
Anti-Hipertensivos
Limite:
Animals
Idioma:
En
Revista:
Bioorg Med Chem Lett
Assunto da revista:
BIOQUIMICA
/
QUIMICA
Ano de publicação:
2011
Tipo de documento:
Article
País de afiliação:
Reino Unido