Ruthenium (II) phosphine/picolinate complexes as antimycobacterial agents

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]PF6 (1), cis- [Ru(pic)(dppe)2]PF6 (2) and [Ru(pic)2(PPh3)2] (3) [pic = 2-pyridinecarboxylate; dppm = bis(diphenylphosphino)methane; dppe = 1,2-bis(diphenylphosphino)ethane; PPh3 = triphenylphosphine] are reported in this article. The complexes were characterized by elemental analysis, spectroscopic and electrochemical techniques. Their in vitro antimycobacterial 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 μg/mL, respectively. The results are comparable to or better than “first line” or “second line” drugs commonly used in the treatment of TB.

Synthesis of cis-[Ru(pic)(dppm)2]PF6 (1) and cis-[Ru(pic)(dppe)2]PF6 (2) by reaction of 2-pyridinecarboxylic acid (pic) with ruthenium (II) diphosphine precursors.Figure optionsDownload as PowerPoint slide