New fluorescent rosamine chelator showing promising antibacterial activity against Gram-positive bacteria
Ângela Novais, Tânia Moniz, Ana Rita Rebelo, Ana M.G.Silva, Maria Rangel, Luísa Peixea
Bioorganic Chemistry
Volume 79, September 2018, Pages 341-349 https://doi.org/10.1016/j.bioorg.2018.05.013

Highlights
• Antibacterial activity assay of diverse 3-hydroxy-4-pyridinone iron chelators.
• Synthesis and characterization of MRB20, a new 3,4-HPO fluorescent iron chelator.
• MRB20 inhibited diverse Gram-positive bacteria species and multidrug resistant strains.
• Promising activity against clinically relevant Staphylococcus and Enterococcus.

Abstract
The restricted number of antibiotics to treat infections caused by common multidrug resistant bacterial pathogens in the clinical setting demands a continuous search for new molecules with antibacterial properties. Bacterial iron deprivation represents a
promising alternative, being iron chelators an attractive class for drug design in which particular compounds seem to have antibacterial effect.

In this work, we report the synthesis and characterization of a new fluorescent 3-hydroxy-4-pyridinone (3,4-HPO) iron chelator functionalized with a carboxyrosamine fluorophore (MRB20). The antibacterial activity of MRB20 was assessed against
representative strains from clinically relevant Gram-positive and Gram-negative bacterial species and further compared with the inhibitory effect of a set of structurally related iron chelators including Deferiprone (1,2-dimethyl-3-hydroxy-4-pyridinone).
Compounds exhibiting a promising minimal inhibitory concentration (MIC < 10 mg/L) were further tested against a wider range of bacterial genera and species (Staphylococcus spp. Enterococcus spp. Listeria monocytogenes, Bacillus spp.), including
multidrug resistant bacteria.

With the exception of the novel compound (MRB20), all chelators inhibited the strains assayed at very high concentrations [minimum inhibitory concentrations (MIC) ranging from 70 mg/L to >180 mg/L]. MRB20 revealed a good antibacterial activity (6.7–
13.2 mg/L) against Gram-positive strains from different genera and species, including clinically relevant species (Staphylococcus aureus, Staphylococcus epidermidis, Enterococcus faecium, Enterococcus faecalis), which might be eventually compatible
with a therapeutic application or as adjuvant.

https://www.sciencedirect.com/science/article/abs/pii/S0045206818301706

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