2-(2-Aminothiazol-4-yl)pyrrolidine-based tartrate diamides as potent, selective and orally bioavailable TACE inhibitors.
Bioorg Med Chem Lett
; 21(10): 3172-6, 2011 May 15.
Article
en En
| MEDLINE
| ID: mdl-21458257
ABSTRACT
TNF-α converting enzyme (TACE) inhibitors are promising agents to treat inflammatory disorders and cancer. We have investigated novel tartrate diamide TACE inhibitors where the tartrate core binds to zinc in a unique tridentate fashion. Incorporating (R)-2-(2-N-alkylaminothiazol-4-yl)pyrrolidines into the left hand side amide of the tartrate scaffold led to the discovery of potent and selective TACE inhibitors, some of which exhibited good rat oral bioavailability.
Texto completo:
1
Banco de datos:
MEDLINE
Asunto principal:
Pirrolidinas
/
Tartratos
/
Inhibidores Enzimáticos
/
Proteínas ADAM
/
Amidas
Límite:
Animals
Idioma:
En
Año:
2011
Tipo del documento:
Article