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 = 3.517.03 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. Biotage 快速纯化制备液相色谱 Flash Isolera one Biotage 快速纯化制备液相色谱 Flash Isolera Prime Biotage 快速纯化制备液相色谱 Flash Isolera LS
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