Nonsteroidal dissociated glucocorticoid agonists containing azaindoles as steroid A-ring mimetics.
J Med Chem
; 53(18): 6681-98, 2010 Sep 23.
Article
in En
| MEDLINE
| ID: mdl-20735001
Syntheses and structure-activity relationships (SAR) of nonsteroidal glucocorticoid receptor (GR) agonists are described. These compounds contain azaindole moieties as A-ring mimetics and display various degrees of in vitro dissociation between gene transrepression and transactivation. Collagen induced arthritis studies in mouse have demonstrated that in vitro dissociated compounds (R)-16 and (R)-37 have steroid-like anti-inflammatory properties with improved metabolic side effect profiles, such as a reduced increase in body fat and serum insulin levels, compared to steroids.
Full text:
1
Collection:
01-internacional
Database:
MEDLINE
Main subject:
Pyridines
/
Pyrroles
/
Steroids
/
Receptors, Glucocorticoid
/
Anti-Inflammatory Agents, Non-Steroidal
Type of study:
Prognostic_studies
Language:
En
Journal:
J Med Chem
Journal subject:
QUIMICA
Year:
2010
Document type:
Article
Affiliation country:
Estados Unidos
Country of publication:
Estados Unidos