4-Aminopyrimidine tetrahydronaphthols: a series of novel vanilloid receptor-1 antagonists with improved solubility properties.
Bioorg Med Chem Lett
; 18(6): 1830-4, 2008 Mar 15.
Article
em En
| MEDLINE
| ID: mdl-18299195
ABSTRACT
8-(6-(4-(Trifluoromethyl)phenyl)pyrimidin-4-ylamino)-1,2,3,4-tetrahydronaphthalen-2-ol (4) and analogs (5-10) were shown to be potent inhibitors of human and rat TRPV1 in vitro with increased solubility over our previous series. Synthesis, SAR, and improvements in metabolic stability and absorption of these compounds are described herein.
Texto completo:
1
Base de dados:
MEDLINE
Assunto principal:
Pirimidinas
/
Canais de Cátion TRPV
/
Naftóis
Limite:
Animals
/
Humans
Idioma:
En
Ano de publicação:
2008
Tipo de documento:
Article