کد مقاله | کد نشریه | سال انتشار | مقاله انگلیسی | نسخه تمام متن |
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1359457 | 981403 | 2010 | 17 صفحه PDF | دانلود رایگان |

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 (IC50 = 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.
Novel C-aryl glucoside SGLT2 inhibitors containing 1,3,4-thiadiazole at the distal ring position were identified as potential antidiabetic agents. A selected compound demonstrated reasonable urinary glucose excretion and glucosuria in normal SD rats along with favorable blood glucose-lowering effects in db/db mice.Figure optionsDownload as PowerPoint slide
Journal: Bioorganic & Medicinal Chemistry - Volume 18, Issue 6, 15 March 2010, Pages 2178–2194