Please use this identifier to cite or link to this item: http://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, 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.
RMID: 0030081281
DOI: 10.1039/c7dt04595f
Appears in Collections:Chemistry publications

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