Exploration of SAR regarding glucose moiety in novel C-aryl glucoside inhibitors of SGLT2.
Bioorg Med Chem Lett
; 21(2): 742-6, 2011 Jan 15.
Article
en En
| MEDLINE
| ID: mdl-21193308
ABSTRACT
In order to investigate SAR regarding glucose moiety in novel C-aryl glucoside SGLT2 inhibitors containing a thiazole motif, a series of chemical modifications on glucose was conducted to explore potential utility as a suitable replacement of glucose per se. Among the compounds prepared, deshydroxy 29 (IC(50)=7.01nM) demonstrated the best in vitro inhibitory activity against SGLT2 in this series to date. But, none of the compounds were better than the parent molecule 5 (IC(50)=1.75nM).
Texto completo:
1
Banco de datos:
MEDLINE
Asunto principal:
Diabetes Mellitus
/
Transportador 2 de Sodio-Glucosa
/
Inhibidores del Cotransportador de Sodio-Glucosa 2
/
Glicósidos
/
Hipoglucemiantes
Límite:
Humans
Idioma:
En
Revista:
Bioorg Med Chem Lett
Asunto de la revista:
BIOQUIMICA
/
QUIMICA
Año:
2011
Tipo del documento:
Article