Synthesis and evaluation of a novel indoledione class of long chain fatty acid elongase 6 (ELOVL6) inhibitors.
J Med Chem
; 52(10): 3142-5, 2009 May 28.
Article
em En
| MEDLINE
| ID: mdl-19388647
ABSTRACT
Novel indoledione derivatives were synthesized and evaluated as long chain fatty acid elongase 6 (ELOVL6) inhibitors. Systematic optimization of an indole class of lead 1 led to the identification of potent ELOVL6 selective inhibitors. Representative inhibitor 37 showed sustained plasma exposure and good liver penetrability in mice. After oral administration, 37 potently inhibited ELOVL6 activity in the liver in mice.
Texto completo:
1
Coleções:
01-internacional
Base de dados:
MEDLINE
Assunto principal:
Acetiltransferases
/
Inibidores Enzimáticos
/
Indóis
Limite:
Animals
Idioma:
En
Ano de publicação:
2009
Tipo de documento:
Article