Spirocyclic ureas: orally bioavailable 11 beta-HSD1 inhibitors identified by computer-aided drug design.
Bioorg Med Chem Lett
; 20(3): 881-6, 2010 Feb 01.
Article
en En
| MEDLINE
| ID: mdl-20064717
ABSTRACT
Structure-guided drug design led to the identification of a class of spirocyclic ureas which potently inhibit human 11beta-HSD1 in vitro. Lead compound 10j was shown to be orally bioavailable in three species, distributed into adipose tissue in the mouse, and its (R) isomer 10j2 was efficacious in a primate pharmacodynamic model.
Texto completo:
1
Bases de datos:
MEDLINE
Asunto principal:
Urea
/
Diseño de Fármacos
/
11-beta-Hidroxiesteroide Deshidrogenasa de Tipo 1
Límite:
Animals
/
Humans
Idioma:
En
Revista:
Bioorg Med Chem Lett
Asunto de la revista:
BIOQUIMICA
/
QUIMICA
Año:
2010
Tipo del documento:
Article
País de afiliación:
Estados Unidos