Imidazopyridine and Pyrazolopiperidine Derivatives as Novel Inhibitors of Serine Palmitoyl Transferase.
J Med Chem
; 59(12): 5904-10, 2016 06 23.
Article
em En
| MEDLINE
| ID: mdl-27213958
ABSTRACT
To develop novel treatments for type 2 diabetes and dyslipidemia, we pursued inhibitors of serine palmitoyl transferase (SPT). To this end compounds 1 and 2 were developed as potent SPT inhibitors in vitro. 1 and 2 reduce plasma ceramides in rodents, have a slight trend toward enhanced insulin sensitization in DIO mice, and reduce triglycerides and raise HDL in cholesterol/cholic acid fed rats. Unfortunately these molecules cause a gastric enteropathy after chronic dosing in rats.
Texto completo:
1
Coleções:
01-internacional
Base de dados:
MEDLINE
Assunto principal:
Piperidinas
/
Pirazóis
/
Piridinas
/
Inibidores Enzimáticos
/
Serina C-Palmitoiltransferase
/
Imidazóis
Limite:
Animals
/
Humans
/
Male
Idioma:
En
Ano de publicação:
2016
Tipo de documento:
Article