Faculdade de Ciências Farmacêuticas, Universidade Estadual Paulista, CEP 14801-902, Araraquara, SP, Brazil.
Eur J Med Chem. 2010 Feb;45(2):598-601. doi: 10.1016/j.ejmech.2009.10.049. Epub 2009 Nov 6.
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 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 microg/mL, respectively. The results are comparable to or better than "first line" or "second line" drugs commonly used in the treatment of TB.
本文报道了三种含有 2-吡啶甲酸阴离子(picolinate)的钌配合物的合成、表征及其抗结核分枝杆菌(MTB)活性。配合物的化学式为 cis-[Ru(pic)(dppm)(2)]PF6(1)、cis-[Ru(pic)(dppe)(2)]PF6(2)和[Ru(pic)(2)(PPh3)2](3)[pic=2-吡啶甲酸;dppm=双(二苯基膦基)甲烷;dppe=1,2-双(二苯基膦基)乙烷;PPh3=三苯基膦]。这些配合物通过元素分析、光谱和电化学技术进行了表征。它们的体外抗分枝杆菌活性通过 REMA 法测定最小抑菌浓度(MIC)来评估。结果表明,配合物(1)和(2)的 MIC 值分别为 0.78 和 0.26μg/mL,活性最佳。这些结果与治疗结核病常用的“一线”或“二线”药物相当或更好。