Design, synthesis, and evaluation of efflux substrate–metal chelator conjugates as potential antimicrobial agents

Maintaining a proper balance of metal concentrations is critical to the survival of bacteria. We have designed and synthesized a series of conjugates of metal chelators and efflux transporter substrates aimed at disrupting bacterial metal homeostasis to achieve bacterial killing. Biological studies showed that two of the compounds had very significant antimicrobial effect with an MIC value of 7.8 μg/mL against Gram-positive Bacillus subtilis.

Graphical abstractA series of efflux substrate–metal chelator conjugates was developed as potential antimicrobial agents.Figure optionsDownload full-size imageDownload as PowerPoint slide