Discovery of Second Generation RORγ Inhibitors Composed of an Azole Scaffold.
J Med Chem
; 62(5): 2837-2842, 2019 03 14.
Article
en En
| MEDLINE
| ID: mdl-30776227
ABSTRACT
Starting from a previously reported RORγ inhibitor (1), successive efforts to improve in vivo potency were continued. Introduction of metabolically beneficial motifs in conjunction with scaffold hopping was examined, resulting in discovery of the second generation RORγ inhibitor composed of a 4-(isoxazol-3-yl)butanoic acid scaffold (24). Compound 24 achieved a 10-fold improvement in in vivo potency in a mouse CD3 challenge model along with significant anti-inflammatory effects in a mouse dermatitis model.
Texto completo:
1
Colección:
01-internacional
Base de datos:
MEDLINE
Asunto principal:
Azoles
/
Miembro 3 del Grupo F de la Subfamilia 1 de Receptores Nucleares
Límite:
Animals
Idioma:
En
Revista:
J Med Chem
Asunto de la revista:
QUIMICA
Año:
2019
Tipo del documento:
Article
País de afiliación:
Japón