Novel C-aryl glucoside SGLT2 inhibitors as potential antidiabetic agents: 1,3,4-Thiadiazolylmethylphenyl glucoside congeners.
Bioorg Med Chem
; 18(6): 2178-2194, 2010 Mar 15.
Article
en En
| MEDLINE
| ID: mdl-20181486
ABSTRACT
Novel C-aryl glucoside SGLT2 inhibitors containing 1,3,4-thiadiazole moieties were designed and synthesized. Among the compounds tested, biaryl-type compounds containing pyrazine 59, 2-furan 61, and 3-thiophene 71 showed the best in vitro inhibitory activities to date (IC(50) = 3.51-7.03 nM) against SGLT2. A selected compound 61, demonstrated reasonable blood glucose-lowering effects, indicating that the information obtained from the SAR studies in this 1,3,4-thiadiazolylmethylphenyl glucoside series might help to design more active SGLT2 inhibitors that are structurally related.
Texto completo:
1
Banco de datos:
MEDLINE
Asunto principal:
Tiadiazoles
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Inhibidores del Cotransportador de Sodio-Glucosa 2
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Glucósidos
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Hipoglucemiantes
Límite:
Animals
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Humans
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Male
Idioma:
En
Revista:
Bioorg Med Chem
Asunto de la revista:
BIOQUIMICA
/
QUIMICA
Año:
2010
Tipo del documento:
Article