Substituted phenyl triazoles as selective inhibitors of 11ß-Hydroxysteroid Dehydrogenase Type 1.
Bioorg Med Chem Lett
; 21(7): 2141-5, 2011 Apr 01.
Article
em En
| MEDLINE
| ID: mdl-21334894
ABSTRACT
3-(Phenylcyclobutyl)-1,2,4-triazoles were identified as inhibitors of 11ß-Hydroxysteroid Dehydrogenase Type 1 (HSD1). They were shown to be active in the mouse in vivo pharmacodynamic model (PD) for HSD1 but exhibited a potent off-target activation of the Pregnane X Receptor (PXR). SAR studies and synthesis of analogs that led to the discovery of a selective HSD1 inhibitor are described in detail.
Texto completo:
1
Base de dados:
MEDLINE
Assunto principal:
Triazóis
/
11-beta-Hidroxiesteroide Desidrogenase Tipo 1
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Inibidores Enzimáticos
Idioma:
En
Ano de publicação:
2011
Tipo de documento:
Article