Discovery and optimization of adamantyl carbamate inhibitors of 11ß-HSD1.
Bioorg Med Chem Lett
; 20(22): 6725-9, 2010 Nov 15.
Article
em En
| MEDLINE
| ID: mdl-20864344
ABSTRACT
Synthesis of 2-adamantyl carbamate derivatives of piperidines and pyrrolidines led to the discovery of 9a with an IC(50) of 15.2 nM against human 11ß-HSD1 in adipocytes. Optimization for increased adipocyte potency, metabolic stability and selectivity afforded 11k and 11l, both of which were >25% orally bioavailable in rat.
Texto completo:
1
Coleções:
01-internacional
Base de dados:
MEDLINE
Assunto principal:
Adamantano
/
11-beta-Hidroxiesteroide Desidrogenase Tipo 1
/
Inibidores Enzimáticos
Limite:
Animals
Idioma:
En
Ano de publicação:
2010
Tipo de documento:
Article