Abstract

AbstractAs the treatment of Staphylococcus aureus infection becomes more and more difficult, it is particularly important to develop new antibacterial agents against S. aureus infection. Herein, three ruthenium (II) complexes containing pyrene groups, [Ru (bpy)2(PYIP)](PF6)2 (Ru‐1), [Ru (dtbpy)2(PYIP)](PF6)2 (Ru‐2), and [Ru (ttbpy)2(PYIP)](PF6)2 (Ru‐3) (PYIP = 2‐(pyren‐1‐yl‐1H‐imidazo[4,5‐f][1,10]phenanthroline, bpy = 2,2′‐bipyridine, dtbpy = 4,4′‐dimethyl‐2,2′‐bipyridine and ttbpy = 4,4′‐di‐tert‐butyl‐2,2′‐bipyridine) were designed and synthesized. The antibacterial activities of them against S. aureus were evaluated by determining the minimum inhibitory concentration and minimum bactericidal concentration. The results showed that three ruthenium complexes had excellent antibacterial activities against S. aureus. Among them, Ru‐2 exhibited the best bacteriostatic concentration and bactericidal activities, which was selected for the further antibacterial mechanism exploring. Ru‐2 can obviously inhibit the growth of bacterial biofilm, and the drug resistance results showed that Ru‐2 can effectively prevent the development of bacterial resistance. Moreover, the in vivo antibacterial activity of Ru‐2 was evaluated by establishing mouse infection model with the results that Ru‐2 could effectively inhibit the growth of bacteria and make mouse wounds heal faster.

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