Optimization of the central linker of dicationic bis-benzimidazole anti-MRSA and anti-VRE agents

A series of bis-benzimidazole diamidine compounds containing different central linkers has been synthesized and evaluated for in vitro antibacterial activities, including drug-resistant bacterial strains. Seven compounds have shown potent antibacterial activities. The anti-MRSA and anti-VRE activities of compound 1h were more potent than that of the lead compound 1a and vancomycin.

Graphical abstractA series of bis-benzimidazole diamidine compounds containing different central linkers has been synthesized and evaluated for in vitro antibacterial activities, including MRSA and VRE bacterial strains.Figure optionsDownload full-size imageDownload as PowerPoint slide