The discovery of potent and selective non-steroidal glucocorticoid receptor modulators, suitable for inhalation.
Bioorg Med Chem Lett
; 24(11): 2571-7, 2014 Jun 01.
Article
en En
| MEDLINE
| ID: mdl-24755427
ABSTRACT
We report the discovery of highly potent and selective non-steroidal glucocorticoid receptor modulators with PK properties suitable for inhalation. A high throughput screen of the AstraZeneca compound collection identified sulfonamide 3 as a potent non-steroidal glucocorticoid receptor ligand. Further optimization of this lead generated indazoles 30 and 48 that were progressed to characterization in in vivo models. X-ray crystallography was used to gain further insight into the binding mode of selected ligands.
Palabras clave
Texto completo:
1
Banco de datos:
MEDLINE
Asunto principal:
Sulfonamidas
/
Receptores de Glucocorticoides
/
Antiinflamatorios no Esteroideos
/
Descubrimiento de Drogas
Límite:
Humans
Idioma:
En
Revista:
Bioorg Med Chem Lett
Asunto de la revista:
BIOQUIMICA
/
QUIMICA
Año:
2014
Tipo del documento:
Article
País de afiliación:
Suecia