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https://hdl.handle.net/2440/112434
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Type: | Journal article |
Title: | Synthesis, isomerisation and biological properties of mononuclear ruthenium complexes containing the bis[4(4′-methyl-2,2′-bipyridyl)]-1,7-heptane ligand |
Author: | Sun, B. Southam, H. Butler, J. Poole, R. Burgun, A. Tarzia, A. Keene, F. Collins, J. |
Citation: | Dalton Transactions: an international journal of inorganic chemistry, 2018; 47(7):2422-2434 |
Publisher: | Royal Society of Chemistry |
Issue Date: | 2018 |
ISSN: | 1477-9226 1477-9234 |
Statement of Responsibility: | Biyun Sun, Hannah M. Southam, Jonathan A. Butler, Robert K. Poole, Alexandre Burgun, Andrew Tarzia, F. Richard Keene and J. Grant Collins |
Abstract: | A series of mononuclear ruthenium(ii) complexes containing the tetradentate ligand bis[4(4'-methyl-2,2'-bipyridyl)]-1,7-heptane have been synthesised and their biological properties examined. In the synthesis of the [Ru(phen')(bb7)]2+ complexes (where phen' = 1,10-phenanthroline and its 5-nitro-, 4,7-dimethyl- and 3,4,7,8-tetramethyl- derivatives), both the symmetric cis-α and non-symmetric cis-β isomers were formed. However, upon standing for a number of days (or more quickly under harsh conditions) the cis-β isomer converted to the more thermodynamically stable cis-α isomer. The minimum inhibitory concentrations (MIC) and the minimum bactericidal concentrations (MBC) of the ruthenium(ii) complexes were determined against six strains of bacteria: Gram-positive Staphylococcus aureus (S. aureus) and methicillin-resistant S. aureus (MRSA); and the Gram-negative Escherichia coli (E. coli) strains MG1655, APEC, UPEC and Pseudomonas aeruginosa (P. aeruginosa). The results showed that the [Ru(5-NO₂phen)(bb₇)]²⁺complex had little or no activity against any of the bacterial strains. By contrast, for the other cis-α-[Ru(phen')(bb₇)]²⁺ complexes, the antimicrobial activity increased with the degree of methylation. In particular, the cis-α-[Ru(Me₄phen)(bb₇)]²⁺ complex showed excellent and uniform MIC activity against all bacteria. By contrast, the MBC values for the cis-α-[Ru(Me₄phen)(bb₇)]²⁺ complex varied considerably across the bacteria and even within S. aureus and E. coli strains. In order to gain an understanding of the relative antimicrobial activities, the DNA-binding affinity, cellular accumulation and water-octanol partition coefficients (log P) of the ruthenium complexes were determined. Interestingly, all the [Ru(phen')(bb7)]²⁺ complexes exhibited stronger DNA binding affinity (Ka ≈ 1 × 10⁷ M⁻¹) than the well-known DNA-intercalating complex [Ru(phen)₂(dppz)]²⁺ (where dppz = dipyrido[3,2-a:2',3'-c]phenazine). |
Description: | Published on 30 January 2018 |
Rights: | This journal is © The Royal Society of Chemistry 2017. Open Access Article. This article is licensed under a Creative Commons Attribution-NonCommercial 3.0 Unported Licence. |
DOI: | 10.1039/c7dt04595f |
Published version: | http://dx.doi.org/10.1039/c7dt04595f |
Appears in Collections: | Aurora harvest 8 Chemistry publications |
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hdl_112434.pdf | Published version | 800.32 kB | Adobe PDF | View/Open |
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