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.
Mark I Lansdell  1 ,  Denise J Burring ,  David Hepworth ,  Matthew Strawbridge ,  Emily Graham ,  Thierry Guyot ,  Mark S Betson ,  James D Hart
Affiliations
  • 1. Pfizer Global Research and Development, Sandwich Laboratories, Ramsgate Road, Kent CT139NJ, UK. [email protected]
PMID: 18755586 DOI: 10.1016/j.bmcl.2008.08.036
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.

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