Metal susceptibility assays and spot plating were used to investigate the antimicrobial activity of enantiopure [Ru(phen) dppz] (phen =1,10-phenanthroline and dppz = dipyrido[3,2-a:2´,3´-c]phenazine) and [μ-bidppz(phen) Ru ] (bidppz =11,11´-bis(dipyrido[3,2-a:2´,3´-c]phenazinyl)), on Gram-negative Escherichia coli and Gram-positive Bacillus subtilis as bacterial models. The minimum inhibitory concentrations (MIC) and minimum bactericidal concentrations (MBC) were determined for both complexes: while [μ-bidppz(phen) Ru ] only showed a bactericidal effect at the highest concentrations tested, the antimicrobial activity of [Ru(phen) dppz] against B. subtilis was comparable to that of tetracyline. In addition, the Δ-enantiomer of [Ru(phen) dppz] showed a 2-fold higher bacteriostatic and bactericidal effect compared to the Λ-enantiomer. This was in accordance with the enantiomers relative binding affinity for DNA, thus strongly indicating DNA binding as the mode of action.
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| http://www.ncbi.nlm.nih.gov/pmc/articles/PMC5248623 | PMC |
| http://dx.doi.org/10.1002/chir.22656 | DOI Listing |
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Synthesis, isomerisation and biological properties of mononuclear ruthenium complexes containing the bis[4(4'-methyl-2,2'-bipyridyl)]-1,7-heptane ligand.
Dalton Trans
February 2018
School of Physical, Environmental and Mathematical Sciences, University of New South Wales, Australian Defence Force Academy, Canberra, ACT 2600, Australia.
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')(bb)] 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.
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