Discovery of phenyl acetic acid substituted quinolines as novel liver X receptor agonists for the treatment of atherosclerosis.
J Med Chem
; 49(21): 6151-4, 2006 Oct 19.
Article
em En
| MEDLINE
| ID: mdl-17034119
ABSTRACT
A structure-based approach was used to optimize our new class of quinoline LXR modulators leading to phenyl acetic acid substituted quinolines 15 and 16. Both compounds displayed good binding affinity for LXRbeta and LXRalpha and were potent activators in LBD transactivation assays. The compounds also increased expression of ABCA1 and stimulated cholesterol efflux in THP-1 cells. Quinoline 16 showed good oral bioavailability and in vivo efficacy in a LDLr knockout mouse model for lesions.
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Base de dados:
MEDLINE
Assunto principal:
Fenilacetatos
/
Quinolinas
/
Receptores Citoplasmáticos e Nucleares
/
Proteínas de Ligação a DNA
/
Aterosclerose
/
Anticolesterolemiantes
Idioma:
En
Ano de publicação:
2006
Tipo de documento:
Article