2014
DOI: 10.1039/c3dt52879k
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Development of ruthenium(ii) complexes as topical antibiotics against methicillin resistant Staphylococcus aureus

Abstract: A series of ruthenium(II) bis(2,2'-bipyridyl) complexes containing N-phenyl-substituted diazafluorenes (Ru-C1, Ru-C6, Ru-C7 and Ru-F) was synthesized and their potential antibacterial activity against methicillin resistant Staphylococcus aureus (MRSA) was investigated. The Ru-C7 complex showed significant improvement in both minimum inhibitory concentration (MIC, 6.25 μg mL(-1)) and minimum bactericidal concentration (MBC, 25 μg mL(-1)) towards MRSA when compared with those of methicillin (positive control) (M… Show more

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Cited by 63 publications
(41 citation statements)
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“…13 [Ru(bpy) 2 (NPDA)] 2+ (NPDA = N -phenyl-substituted diazofluorene) is active against methicillin-resistant S. aureus (MRSA) and generates ROS to kill MRSA. 14 Some dinuclear Ru( ii ) complexes have been studied, where rigid linkers between metal centers show lower activity against S. aureus and E. coli compared to flexible linkers. 15 The activity appeared to be linked to lipophilicity, as increased lipophilicity results in increased penetration through cell membranes and therefore increased uptake.…”
Section: Introductionmentioning
confidence: 99%
“…13 [Ru(bpy) 2 (NPDA)] 2+ (NPDA = N -phenyl-substituted diazofluorene) is active against methicillin-resistant S. aureus (MRSA) and generates ROS to kill MRSA. 14 Some dinuclear Ru( ii ) complexes have been studied, where rigid linkers between metal centers show lower activity against S. aureus and E. coli compared to flexible linkers. 15 The activity appeared to be linked to lipophilicity, as increased lipophilicity results in increased penetration through cell membranes and therefore increased uptake.…”
Section: Introductionmentioning
confidence: 99%
“…Several other N−N ruthenium(II) complexes have also been shown to permeabilize bacterial membranes . However, other antibacterial ruthenium(II) complexes have been shown to produce reactive oxygen species (ROS), interact with proteins or bind to nucleic acids (DNA,, and RNA). As such, the exact biological mode of action of the known ruthenium(II) antibacterial complexes has still not been completely elucidated .…”
Section: Resultsmentioning
confidence: 99%
“…Recently Ru(II) complexes [Ru(L 14 )(bpy) 2 ](PF 6 ) 2 (where L 14 is a 4,5-diazafluoren-9-imine ligand with various N-aryl groups) have been found to be effective topical antibiotics against the bacteria Staphylococcus aureus which is resistant to the antibiotic methicillin. 167 In particular the derivative with a -OC 7 H 15 group attached to the N-aryl group, which is nontoxic toward human skin keratinocyte cells, exhibits strong microbicidal and bacterial growth inhibitory effects. 167 One possible mechanism, for how these Ru(II) complexes are active against S. aureus, is through the generation of reactive oxygen species.…”
Section: Iii4 Bioinorganic Chemistry Of 45-diazafluorene Derivativesmentioning
confidence: 99%