Deferasirox (ExJade): A Fluorescent Pro-Chelator Active Against Antibiotic Resistant Bacteria
2020
Deferasirox,
ExJade, an FDA-approved treatment for iron overload disorders has been
shown to inhibit the growth of both gram-positive and -negative bacteria
through iron (Fe(III)) chelation. Modification of the ExJade framework led to the identification
of a new fluorescent platform ExPh and
ExBT. Functionalization of the
phenol moieties on ExBT with
phosphate units afforded a ratiometric fluorescent pro-chelator (ExPhos),
which was effective in the inhibition of two clinically relevant
antibiotic-resistant bacteria, (MRSA (ATCC 43300) and VRE (ATCC 51299)), and
allowed the fluorescent imaging of MRSA. Remarkably,
this pro-chelation strategy proved selective towards bacteria with no
cytotoxicity observed for ExPhos treated A549 cells (72 h incubation). This
work represents a new pro-chelator antibiotic strategy that can be modified
with a chosen reactive chemical trigger to provide a diagnostic signal in
conjunction with a therapeutic response with a potential of minimal
off-target toxicities.
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