Auranofin, (AF), a gold(I) complex in clinical use for the therapy of rheumatoid arthritis, is reported here to produce remarkable bactericidal effects in vitro against Staphylococcus sp. Noticeably, a similar antimicrobial action and potency are also noticed toward a few methicillin-resistant Staphylococcus aureus strains but not toward Escherichia coli. The time and concentration dependencies of the antimicrobial actions of AF have been characterized through recording time kill curves, and a concentration dependent profile highlighted. Overall, the present results point out that auranofin might be quickly and successfully repurposed for the treatment of severe bacterial infections due to resistant Staphylococci.
Due to the so‐called “antibiotic resistance crisis” new antibacterial agents are urgently sought to treat multidrug‐resistant pathogens. A group of gold‐ or silver‐based complexes, of general formula [M(PEt3)X] (with M=Au or Ag, and X=Cl, Br or I), alongside with three complexes bearing a positive or negative charge—[Au(PEt3)2]Cl, K[Au(CN)2] and [Ag(PEt3)2]NO3—were prepared and comparatively tested with auranofin on a representative panel of pathogens including Gram‐positive, Gram‐negative and Candida strains. Interestingly, all the gold and silver complexes tested were active on Gram‐positive strains, with the gold complexes having greater efficacy. The effects of the gold compounds were potentiated to a larger extent than silver compounds when tested in combination with a permeabilizing agent. A number of relevant structure–activity relationships emerged from the comparative analysis of the observed antibacterial profiles, shedding new light on the underlying molecular mechanisms of the action of these compounds.
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