Novel C-aryl glucoside SGLT2 inhibitors as potential antidiabetic agents: Pyridazinylmethylphenyl glucoside congeners.

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Kim MJ, Lee J, Kang SY, Lee SH, Son EJ, Jung ME, Lee SH, Song KS, Lee M, Han HK, Kim J, Lee J

Novel C-aryl glucoside SGLT2 inhibitors as potential antidiabetic agents: Pyridazinylmethylphenyl glucoside congeners.

Bioorg Med Chem Lett. 2010 Jun 1;20(11):3420-5. doi: 10.1016/j.bmcl.2010.04.006. Epub 2010 Apr 9.

PubMed ID
20434909 [ View in PubMed
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Abstract

Novel C-aryl glucoside SGLT2 inhibitors containing pyridazine motif were designed and synthesized for biological evaluation. Among the compounds tested, pyridazine containing methylthio moiety 22l or thiadiazole ring 22ah showed the best in vitro inhibitory activities in this series (IC(50)=13.4, 11.4nM, respectively) against SGLT2 to date. Subsequently, compound 22l exhibited reasonable urinary glucose excretion and glucosuria in normal SD rats, thereby demonstrating that this pyridazine series possesses both in vitro SGLT2 inhibition and in vivo efficacy, albeit to a lower degree.

DrugBank Data that Cites this Article

Binding Properties
DrugTargetPropertyMeasurementpHTemperature (°C)
DapagliflozinSodium/glucose cotransporter 2IC 50 (nM)0.49N/AN/ADetails