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
in En
| 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.
Full text:
1
Collection:
01-internacional
Database:
MEDLINE
Main subject:
11-beta-Hydroxysteroid Dehydrogenase Type 1
/
Enzyme Inhibitors
/
Isoquinolines
Limits:
Animals
/
Humans
Language:
En
Journal:
Bioorg Med Chem Lett
Journal subject:
BIOQUIMICA
/
QUIMICA
Year:
2011
Document type:
Article
Affiliation country: