Synthesis and structure–activity relationship of dicationic diaryl ethers as novel potent anti-MRSA and anti-VRE agents

A series of dicationic diaryl ethers have been synthesized and evaluated for in vitro antibacterial activities, including drug resistant bacterial strains. Most of these compounds have shown potent antibacterial activities. Several compounds, such as piperidinyl and thiomorpholinyl compounds 9e and 9l, improved the antimicrobial selectivity and kept potent anti-MRSA and anti-VRE activity. The most potent bis-indole diphenyl ether 19 exhibited anti-MRSA MIC value of ⩽0.06 μg/mL and enhanced antimicrobial selectivity.

Graphical abstractA series of dicationic diaryl ethers have been synthesized and evaluated for in vitro antibacterial activities, including MRSA and VRE bacterial strains.Figure optionsDownload full-size imageDownload as PowerPoint slide