Two perfectly cromulent ferrocene containing ruthenium(II)-arene antibacterial agents

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The overuse and misuse of antibiotics are contributing factors that has led to the evolution of virulent bacterial strains that are resistant to first-line treatments. This has necessitated the development of novel agents to treat such pathogens, for which metal complexes have shown promise. In particular, the incorporation of ferrocene into a biologically active scaffold has shown documented success. Within this report, a series of three Ru-arene complexes with chelating 1,4-substituted 1,2,3-triazole ligands were synthesized and evaluated for their respective antibacterial activity against three clinically-relevant bacterial strains. Taken together, the subtle changes made to the ligands allowed for the determination of structure–activity relationships, where the inclusion of a ferrocene proved critical for antibacterial activity. Furthermore, the methyl group on the linker for complex RuTMFc embiggened its lipophilicity and protein binding, while the radical scavenging ability of the complex was diminished relative to RuTHFc that had unsubstituted hydrocarbon linker. This culminated with RuTMFc having the greatest antibacterial activity observed for all three complexes, while also exhibiting the lowest hemolytic activity.