C-aryl glucosides substituted at the 4'-position as potent and selective renal sodium-dependent glucose co-transporter 2 (SGLT2) inhibitors for the treatment of type 2 diabetes.
Bioorg Med Chem Lett
; 21(15): 4465-70, 2011 Aug 01.
Article
en En
| MEDLINE
| ID: mdl-21737266
ABSTRACT
A series of C-aryl glucosides with various substituents at the 4'-position of the distal aryl ring have been synthesized and evaluated for inhibition of hSGLT1 and hSGLT2. Introduction of alkyl or alkoxy substituents at the 4'-position was found to improve SGLT2 potency, whereas introduction of a hydrophilic group at this position was deleterious. Compounds with alkoxy-, cycloalkoxy- or cycloalkenyloxy-ethoxy scaffolds exhibited good inhibitory activity and high selectivity toward SGLT2. Selected compounds were investigated for in vivo efficacy.
Texto completo:
1
Bases de datos:
MEDLINE
Asunto principal:
Diabetes Mellitus Tipo 2
/
Inhibidores del Cotransportador de Sodio-Glucosa 2
/
Glucósidos
/
Hipoglucemiantes
Límite:
Humans
Idioma:
En
Revista:
Bioorg Med Chem Lett
Asunto de la revista:
BIOQUIMICA
/
QUIMICA
Año:
2011
Tipo del documento:
Article