Design and synthesis of fluorescent SGLT2 inhibitors.
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.
Lansdell
Mark I
MI
Pfizer Global Research and Development, Sandwich Laboratories, Ramsgate Road, Kent CT139NJ, UK. mark.lansdell@pfizer.com
Burring
Denise J
DJ
Hepworth
David
D
Strawbridge
Matthew
M
Graham
Emily
E
Guyot
Thierry
T
Betson
Mark S
MS
Hart
James D
JD