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

Authors :
Pavan, Fernando R.
Poelhsitz, Gustavo V.
Barbosa, Marilia I.F.
Leite, Sergio R.A.
Batista, Alzir A.
Ellena, Javier
Sato, Leticia S.
Franzblau, Scott G.
Moreno, Virtudes
Gambino, Dinorah
Leite, Clarice Q.F.
Source :
European Journal of Medicinal Chemistry. Oct2011, Vol. 46 Issue 10, p5099-5107. 9p.
Publication Year :
2011

Abstract

Abstract: 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. [Copyright &y& Elsevier]

Details

Language :
English
ISSN :
02235234
Volume :
46
Issue :
10
Database :
Academic Search Index
Journal :
European Journal of Medicinal Chemistry
Publication Type :
Academic Journal
Accession number :
65935454
Full Text :
https://doi.org/10.1016/j.ejmech.2011.08.023