SAR and optimization of thiazole analogs as potent stearoyl-CoA desaturase inhibitors.
Bioorg Med Chem Lett
; 20(5): 1593-7, 2010 Mar 01.
Article
en En
| MEDLINE
| ID: mdl-20137926
ABSTRACT
Elevated stearoyl-CoA desaturase (SCD) activity has been linked to a number of metabolic disorders including obesity and type II diabetes. Compound 3j, a potent SCD inhibitor (human HepG2 IC(50)=1nM) was identified from the optimization of a lead thiazole compound MF-152 with over 100-fold improvement in potency. In a 4-week chronic oral dosing at 0.2mg/kg, 3j gave a robust 24% prevention of body weight gain in mice fed on a high fat diet accompanied with an improved metabolic profile on insulin and glucose levels.
Texto completo:
1
Colección:
01-internacional
Banco de datos:
MEDLINE
Asunto principal:
Oxadiazoles
/
Estearoil-CoA Desaturasa
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Tiazoles
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Inhibidores Enzimáticos
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Hipoglucemiantes
Límite:
Animals
/
Humans
Idioma:
En
Revista:
Bioorg Med Chem Lett
Asunto de la revista:
BIOQUIMICA
/
QUIMICA
Año:
2010
Tipo del documento:
Article