Design of a potent, soluble glucokinase activator with increased pharmacokinetic half-life.
Bioorg Med Chem Lett
; 21(11): 3467-70, 2011 Jun 01.
Article
en En
| MEDLINE
| ID: mdl-21515051
ABSTRACT
The continued optimization of a series of glucokinase activators is described, including attempts to understand the interplay between molecular structure and the composite parameter of unbound clearance. These studies resulted in the discovery of a new scaffold for glucokinase activators and further exploration of this scaffold led to the identification of GKA60. GKA60 maintains an excellent balance of potency and physical properties whilst possessing a significantly different, but complimentary, pre-clinical pharmacokinetic profile compared with the previously disclosed compound GKA50.
Texto completo:
1
Colección:
01-internacional
Base de datos:
MEDLINE
Asunto principal:
Diseño de Fármacos
/
Activadores de Enzimas
/
Activación Enzimática
/
Glucoquinasa
/
Hipoglucemiantes
Límite:
Animals
/
Humans
Idioma:
En
Revista:
Bioorg Med Chem Lett
Asunto de la revista:
BIOQUIMICA
/
QUIMICA
Año:
2011
Tipo del documento:
Article
País de afiliación:
Reino Unido