Optimization of oxadiazole derivatives with a spirocyclic cyclohexane structure as novel GPR119 agonists.
Bioorg Med Chem Lett
; 29(16): 2100-2106, 2019 08 15.
Article
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| MEDLINE
| ID: mdl-31288965
ABSTRACT
We describe here a novel GPR119 agonist 24, which showed a potent and long-acting hypoglycemic effect in rats via oral dosing. For the discovery of 24, we chose compound 5, which possessed an oxadiazole linker, as a lead compound among our spirocyclic cyclohexane GPR119 agonist series, taking into account its lower plasma protein binding nature. 3,5-Difluoro and 4-methylsulfonylmethy groups on the left side phenyl group, and a gem-difluoro group on the right side of 24 are important for its agonist potency and metabolic stability, respectively.
Palabras clave
Texto completo:
1
Banco de datos:
MEDLINE
Asunto principal:
Oxadiazoles
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Compuestos de Espiro
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Ciclohexanos
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Receptores Acoplados a Proteínas G
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Hipoglucemiantes
Límite:
Animals
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Humans
Idioma:
En
Año:
2019
Tipo del documento:
Article