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(Referência obtida automaticamente do Web of Science, por meio da informação sobre o financiamento pela FAPESP e o número do processo correspondente, incluída na publicação pelos autores.)

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

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Autor(es):
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Pavan, Fernando R. [1] ; Poelhsitz, Gustavo V. [2] ; Barbosa, Marilia I. F. [3] ; Leite, Sergio R. A. [4] ; Batista, Alzir A. [3] ; Ellena, Javier [5] ; Sato, Leticia S. [1] ; Franzblau, Scott G. [6] ; Moreno, Virtudes [7] ; Gambino, Dinorah [8] ; Leite, Clarice Q. F. [1]
Número total de Autores: 11
Afiliação do(s) autor(es):
[1] Univ Estadual Paulista, Fac Ciencias Farmaceut, BR-14801902 Araraquara, SP - Brazil
[2] Univ Fed Uberlandia, Inst Quim, BR-38400902 Uberlandia, MG - Brazil
[3] Univ Fed Sao Carlos, Dept Quim, BR-13565905 Sao Carlos, SP - Brazil
[4] Univ Estadual Paulista, Inst Quim, BR-14800900 Araraquara, SP - Brazil
[5] Univ Sao Paulo, Inst Fis Sao Carlos, BR-13560970 Sao Carlos, SP - Brazil
[6] Univ Illinois, Coll Pharm, Inst TB Res, Chicago, IL - USA
[7] Univ Barcelona, Dept Quim Inorgan, E-08028 Barcelona - Spain
[8] Univ Republica, Fac Quim, Catedra Quim Inorgan, Dept Estrella Campos, Montevideo 11800 - Uruguay
Número total de Afiliações: 8
Tipo de documento: Artigo Científico
Fonte: EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY; v. 46, n. 10, p. 5099-5107, OCT 2011.
Citações Web of Science: 53
Resumo

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)]PF(6) (SCAR01), {[}Ru(pic)(dppb) (Me-bipy)]PF(6) (SCAR02), {[}Ru(Pic)(dPPb)(Cl-bipy]PF(6) (SCAR03) and {[}Ru(pic)(dppb)(phen)]PF(6) (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)]PF(6)(SCAR05) and cis-{[}RuCl(2)(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. (AU)

Processo FAPESP: 08/10390-2 - Determinação do perfil pré-clínico da atividade antituberculose in vitro e in vivo dos complexos de rutênio(II)fosfinas / diiminas
Beneficiário:Fernando Rogério Pavan
Linha de fomento: Bolsas no Brasil - Doutorado