Discovery of 3-hydroxy-4-cyano-isoquinolines as novel, potent, and selective inhibitors of human 11ß-hydroxydehydrogenase 1 (11ß-HSD1).
Bioorg Med Chem Lett
; 21(22): 6693-8, 2011 Nov 15.
Article
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| MEDLINE
| ID: mdl-21983444
ABSTRACT
Derived from the HTS hit 1, a series of hydroxyisoquinolines was discovered as potent and selective 11ß-HSD1 inhibitors with good cross species activity. Optimization of substituents at the 1 and 4 positions of the isoquinoline group in addition to the core modifications, with a special focus on enhancing metabolic stability and aqueous solubility, resulted in the identification of several compounds as potent advanced leads.
Texto completo:
1
Banco de datos:
MEDLINE
Asunto principal:
11-beta-Hidroxiesteroide Deshidrogenasa de Tipo 1
/
Inhibidores Enzimáticos
/
Isoquinolinas
Límite:
Animals
/
Humans
Idioma:
En
Revista:
Bioorg Med Chem Lett
Asunto de la revista:
BIOQUIMICA
/
QUIMICA
Año:
2011
Tipo del documento:
Article
País de afiliación:
Estados Unidos