Novel macrocyclic C-aryl glucoside SGLT2 inhibitors as potential antidiabetic agents.

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Kim MJ, Lee SH, Park SO, Kang H, Lee JS, Lee KN, Jung ME, Kim J, Lee J

Novel macrocyclic C-aryl glucoside SGLT2 inhibitors as potential antidiabetic agents.

Bioorg Med Chem. 2011 Sep 15;19(18):5468-79. doi: 10.1016/j.bmc.2011.07.045. Epub 2011 Jul 28.

PubMed ID

21868239 [ View in PubMed

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Abstract

Novel macrocyclic C-aryl glucoside SGLT2 inhibitors were designed and synthesized. Two different synthetic routes of macrocyclization were adopted to prepare novel ansa SGLT2 inhibitors. Among the compounds tested, [1,7]dioxacyclopentadecine macrocycles possessing methylthiophenyl at the distal ring 40 or ethoxyphenyl at the distal ring 23 showed the best in vitro inhibitory activity in this series to date (40, IC(50)=0.778 nM and 23, IC(50)=0.899 nM) against hSGLT2.

DrugBank Data that Cites this Article

Binding Properties

Drug	Target	Property	Measurement	pH	Temperature (°C)
Dapagliflozin	Sodium/glucose cotransporter 2	IC 50 (nM)	1.35	N/A	N/A	Details