Bicyclic heteroaryl inhibitors of stearoyl-CoA desaturase: from systemic to liver-targeting inhibitors.
Bioorg Med Chem Lett
; 21(19): 5692-6, 2011 Oct 01.
Article
em En
| MEDLINE
| ID: mdl-21871798
ABSTRACT
Optimization of a lead thiazole amide MF-152 led to the identification of potent bicyclic heteroaryl SCD1 inhibitors with good mouse pharmacokinetic profiles. In a view to target the liver for efficacy and to avoid SCD1 inhibition in the skin and eyes where adverse effects were previously observed in rodents, representative systemically-distributed SCD1 inhibitors were converted into liver-targeting SCD1 inhibitors.
Texto completo:
1
Base de dados:
MEDLINE
Assunto principal:
Piperazinas
/
Estearoil-CoA Dessaturase
/
Tiazóis
/
Desenho de Fármacos
/
Inibidores Enzimáticos
/
Descoberta de Drogas
Idioma:
En
Ano de publicação:
2011
Tipo de documento:
Article