Azabenzthiazole inhibitors of leukotriene A4 hydrolase.
Bioorg Med Chem Lett
; 22(24): 7504-11, 2012 Dec 15.
Article
en En
| MEDLINE
| ID: mdl-23127888
ABSTRACT
Previously, benzthiazole containing LTA(4)H inhibitors were discovered that were potent (1-3), but were associated with the potential for a hERG liability. Utilizing medicinal chemistry first principles (e.g., introducing rigidity, lowering cLogD) a new benzthiazole series was designed, congeners of 1-3, which led to compounds 7a, 7c, 12a-d which exhibited LTA(4)H IC(50)=3-6 nM and hERG Dofetilide Binding IC(50)=8.9-> >10 µM.
Texto completo:
1
Bases de datos:
MEDLINE
Asunto principal:
Compuestos Aza
/
Inhibidores Enzimáticos
/
Epóxido Hidrolasas
/
Benzotiazoles
Límite:
Animals
/
Humans
Idioma:
En
Revista:
Bioorg Med Chem Lett
Asunto de la revista:
BIOQUIMICA
/
QUIMICA
Año:
2012
Tipo del documento:
Article
País de afiliación:
Estados Unidos