Design and synthesis of fluorescent SGLT2 inhibitors

Bioorg Med Chem Lett. 2008 Sep 15;18(18):4944-7. doi: 10.1016/j.bmcl.2008.08.036. Epub 2008 Aug 14.

Abstract

The design and synthesis of the first fluorophore-conjugated SGLT2 inhibitors is described. The mode of linking the fluorophore to the SGLT2 pharmacophore was found to be crucial in achieving optimum potency. Superior potency to phlorizin was provided by examples containing TAMRA, BODIPY, Cy3B and NBD fluorophores.

MeSH terms

  • Combinatorial Chemistry Techniques
  • Drug Design
  • Fluorescent Dyes / chemical synthesis*
  • Fluorescent Dyes / chemistry
  • Fluorescent Dyes / pharmacology*
  • Molecular Structure
  • Phlorhizin / pharmacology
  • Sodium-Glucose Transporter 2 Inhibitors*

Substances

  • Fluorescent Dyes
  • Sodium-Glucose Transporter 2 Inhibitors
  • Phlorhizin