Ruthenium (II) phosphine/picolinate complexes as antimycobacterial agents

Author(s)

Pavan, Fernando R. ^[1] ; Von Poelhsitz, Gustavo ^[2] ; do Nascimento, Fabio B. ^[3] ; Leite, Sergio R. A. ^[4] ; Batista, Alzir A. ^[3] ; Deflon, Victor M. ^[5] ; Sato, Daisy N. ^[6] ; Franzblau, Scott G. ^[7] ; Leite, Clarice Q. F. ^[1]

Affiliation

^[1] Univ Estadual Paulista, Fac Ciencias Farmaceut, BR-14801902 Araraquara, SP - Brazil

^[2] Univ Fed Goias, Dept Quim, BR-75704020 Catalao, Go - 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 Quim Sao Carlos, BR-13566590 Sao Carlos, SP - Brazil

^[6] Inst Adolfo Lutz Registro, Unidade Ribeirao Preto, BR-14085410 Ribeirao Preto, SP - Brazil

^[7] Univ Illinois, Coll Pharm, Inst TB Res, Chicago, IL - USA

• Document type: Journal article
• Source: EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY; v. 45, n. 2, p. 598-601, FEB 2010.
• Web of Science Citations: 35

Abstract

The synthesis, characterization and the anti-Mycobacterium tuberculosis (MTB) activities of three ruthenium complexes containing the 2-pyridinecarboxylic acid anion (picolinate), with formulae cis-{[}Ru(pic)(dppm)(2)]PF(6) (1), Cis- {[}Ru(pic)(dppe)(2)]PF(6) (2) and {[}Ru(pic)(2)(PPh(3))(2)] (3) {[}pic = 2-pyridinecarboxylate; dppm = bis(diphenylphosphino)methane: dppe = 1,2-bis(diphenylphosphino)ethane; PPh(3) = triphenylphosphine] are reported in this article. The complexes were characterized by elemental analysis, spectroscopic and electrochemical techniques. Their in vitro anti mycobacterial activity was determinated as the Minimum Inhibitory Concentration (MIC) for MTB cell growth, measured by the REMA method. The best MICs were found for complexes (1) and (2), with values of 0.78 and 0.26 mu g/mL, respectively. The results are comparable to or better than ``first line{''} or ``second line{''} drugs commonly used in the treatment of TB. (C) 2009 Elsevier Masson SAS. All rights reserved. (AU)

• FAPESP's process: 08/10390-2 - Determination of pre-clinical profile in vitro and in vivo anti-tuberculosis activity of ruthenium(II)phosphine / picolinate complexes
• Grantee: Fernando Rogério Pavan
• Support Opportunities: Scholarships in Brazil - Doctorate