Discovery and optimization of a series of liver X receptor antagonists.
Bioorg Med Chem Lett
; 22(18): 5966-70, 2012 Sep 15.
Article
em En
| MEDLINE
| ID: mdl-22901900
ABSTRACT
The present report describes our efforts to convert an existing LXR agonist into an LXR antagonist using a structure-based approach. A series of benzenesulfonamides was synthesized based on structural modification of a known LXR agonist and was determined to be potent dual liver X receptor (LXR α/ß) ligands. Herein we report the identification of compound 54 as the first reported LXR antagonist that is suitable for pharmacological in vivo evaluation in rodents.
Texto completo:
1
Coleções:
01-internacional
Base de dados:
MEDLINE
Assunto principal:
Sulfonamidas
/
Descoberta de Drogas
/
Receptores Nucleares Órfãos
Limite:
Animals
/
Humans
/
Male
Idioma:
En
Ano de publicação:
2012
Tipo de documento:
Article