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]
- 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