Ruthenium(II) phosphine/diimine/picolinate complexes: Inorganic compounds as agents against tuberculosis
Contribuinte(s) |
Universidade Estadual Paulista (UNESP) |
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Data(s) |
20/05/2014
20/05/2014
01/10/2011
|
Resumo |
Conselho Nacional de Desenvolvimento Científico e Tecnológico (CNPq) Fundação de Amparo à Pesquisa do Estado de São Paulo (FAPESP) Processo FAPESP: 08/10390-2 Processo FAPESP: 09/06499-1 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. |
Formato |
5099-5107 |
Identificador |
http://dx.doi.org/10.1016/j.ejmech.2011.08.023 European Journal of Medicinal Chemistry. Paris: Elsevier France-editions Scientifiques Medicales Elsevier, v. 46, n. 10, p. 5099-5107, 2011. 0223-5234 http://hdl.handle.net/11449/7486 10.1016/j.ejmech.2011.08.023 WOS:000296041600033 |
Idioma(s) |
eng |
Publicador |
Elsevier France-editions Scientifiques Medicales Elsevier |
Relação |
European Journal of Medicinal Chemistry |
Direitos |
closedAccess |
Palavras-Chave | #Mycobacterium tuberculosis #Drug resistance #Ruthenium #Phosphine/diimine/picolinate |
Tipo |
info:eu-repo/semantics/article |