Discovery of diamide compounds as diacylglycerol acyltransferase 1 (DGAT1) inhibitors.
Bioorg Med Chem Lett
; 26(4): 1245-8, 2016 Feb 15.
Article
en En
| MEDLINE
| ID: mdl-26804232
ABSTRACT
Diamide compounds were identified as potent DGAT1 inhibitors in vitro, but their poor molecular properties resulted in low oral bioavailability, both systemically and to DGAT1 in the enterocytes of the small intestine, resulting in a lack of efficacy in vivo. Replacing an N-alkyl group on the diamide with an N-aryl group was found to be an effective strategy to confer oral bioavailability and oral efficacy in this lipophilic diamide class of inhibitors.
Palabras clave
Texto completo:
1
Colección:
01-internacional
Base de datos:
MEDLINE
Asunto principal:
Diamida
/
Inhibidores Enzimáticos
/
Diacilglicerol O-Acetiltransferasa
Límite:
Animals
/
Humans
Idioma:
En
Revista:
Bioorg Med Chem Lett
Asunto de la revista:
BIOQUIMICA
/
QUIMICA
Año:
2016
Tipo del documento:
Article
País de afiliación:
Estados Unidos