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
in 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.
Full text:
1
Collection:
01-internacional
Database:
MEDLINE
Main subject:
Thiadiazoles
/
Sodium-Glucose Transporter 2 Inhibitors
/
Glucosides
/
Hypoglycemic Agents
Limits:
Animals
/
Humans
/
Male
Language:
En
Journal:
Bioorg Med Chem
Journal subject:
BIOQUIMICA
/
QUIMICA
Year:
2010
Type:
Article