Synthesis and pharmacological validation of a novel series of non-steroidal FXR agonists.
Bioorg Med Chem Lett
; 20(16): 4911-7, 2010 Aug 15.
Article
em En
| MEDLINE
| ID: mdl-20638278
ABSTRACT
To overcome the known liabilities of GW4064 a series of analogs were synthesized where the stilbene double bond is replaced by an oxymethylene or amino-methylene linker connecting a terminal benzoic acid with a substituted heteroaryl in the middle ring position. As a result we discovered compounds with increased potency in vitro that cause dose-dependent reduction of plasma triglycerides and cholesterol in db/db mice down to 2 x 1 mg/kg/day upon oral administration.
Texto completo:
1
Coleções:
01-internacional
Base de dados:
MEDLINE
Assunto principal:
Receptores Citoplasmáticos e Nucleares
/
Fármacos Antiobesidade
/
Isoxazóis
Limite:
Animals
Idioma:
En
Ano de publicação:
2010
Tipo de documento:
Article