2-Arylbenzoxazoles as CETP inhibitors: raising HDL-C in cynoCETP transgenic mice.
Bioorg Med Chem Lett
; 21(1): 558-61, 2011 Jan 01.
Article
en En
| MEDLINE
| ID: mdl-21094047
ABSTRACT
We describe structure-activity studies leading to the discovery of 2-arylbenzoxazole 3, the first in a series to raise serum high-density lipoprotein cholesterol levels in transgenic mice. Replacement of the 4-piperidinyloxy moiety with piperazinyl provided a more synthetically tractable lead, which upon optimization resulted in compound 4, an excellent inhibitor of cholesteryl ester transfer protein function with good pharmacokinetic properties and in vivo efficacy.
Texto completo:
1
Colección:
01-internacional
Base de datos:
MEDLINE
Asunto principal:
Benzoxazoles
/
Proteínas de Transferencia de Ésteres de Colesterol
/
HDL-Colesterol
/
Acetanilidas
Límite:
Animals
Idioma:
En
Revista:
Bioorg Med Chem Lett
Asunto de la revista:
BIOQUIMICA
/
QUIMICA
Año:
2011
Tipo del documento:
Article
País de afiliación:
Estados Unidos