Ruthenium(II) phosphine/diimine/picolinate complexes: Inorganic compounds as agents against tuberculosis

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Elsevier France-editions Scientifiques Medicales Elsevier


This paper describes the synthesis and characterization of four new ruthenium complexes containing 1,4 bis(diphenylphosphino)butane (dppb), 2-pyridinecarboxylic acid anion (pic) and the diimines [(2,2'-bipyridine (bipy), 4,4'-dimethyl-2,2'-bipyridine (Me-bipy), 4,4'-dichloro-2,2'-bipyridine (Cl-bipy) and 1,10-phenanthroline (phen) as ligands, with formulae [Ru(pic)(dppb)(bipy)]PF6 (SCAR01), [Ru(pic)(dppb) (Me-bipy)]PF6 (SCAR02), [Ru(Pic)(dPPb)(Cl-bipy]PF6 (SCAR03) and [Ru(pic)(dppb)(phen)]PF6 (SCAR04). Additionally, the in vitro anti-Mycobacterium tuberculosis (MTB) activity, cytotoxicity and activity against in vitro infection of these complexes and two more complexes, cis-[Ru(pic)(dppe)(2)]PF6(SCAR05) and cis-[RuCl2(dppb)(bipy)] (SCAR06), and their free ligands are described and discussed. All compounds showed excellent MIC against MTB, low cytotoxicity and a selectivity index higher than 10. Also, all compounds showed significant intracellular inhibition and the compound SCAR05 showed a better activity than rifampin and SQ109. This is the first report of activity against in vitro infection of ruthenium compounds. (C) 2011 Elsevier Masson SAS. All rights reserved.



Mycobacterium tuberculosis, Drug resistance, Ruthenium, Phosphine/diimine/picolinate

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European Journal of Medicinal Chemistry. Paris: Elsevier France-editions Scientifiques Medicales Elsevier, v. 46, n. 10, p. 5099-5107, 2011.