Facultad de Química, Universidad de la República, Gral. Flores 2124, C.C. 1157, Montevideo 11800, Uruguay.
Eur J Med Chem. 2009 Dec;44(12):4937-43. doi: 10.1016/j.ejmech.2009.08.008. Epub 2009 Aug 29.
In the search of new therapeutic tools for the treatment of American Trypanosomiasis, the largest parasitic disease burden in the American continent, three series of novel ruthenium complexes of the formula [RuCl(2)(HL)(2)], [RuCl(3)(dmso)(HL)] and [RuCl(PPh(3))(L)(2)] with bioactive 5-nitrofuryl containing thiosemicarbazones as ligands (HL neutral, L monoanionic) were synthesized and characterized. Their in vitro growth inhibition activity against Trypanosoma cruzi and the effect of co-ligands in related physicochemical properties i.e. nitro moiety redox potential, lipophilicity and free radical scavenger capacity were evaluated. Results show that although a loss of activity was observed as a consequence of ruthenium complexation, lipophilicity and free radical scavenger capacity of the obtained complexes could be correlated to their trypanocidal effect.
在寻找治疗美洲锥虫病（美洲大陆负担最重的寄生虫病）的新治疗工具的过程中，我们合成并表征了三种新型钌配合物系列：[RuCl(2)(HL)(2)]、[RuCl(3)(dmso)(HL)]和[RuCl(PPh(3))(L)(2)]，配体为具有生物活性的含 5-硝基糠基的硫代缩氨基脲（HL 为中性，L 为单阴离子）。评估了它们对 Trypanosoma cruzi 的体外生长抑制活性以及辅助配体在相关物理化学性质（如硝基部分氧化还原电位、亲脂性和自由基清除能力）中的作用。结果表明，尽管钌配合物的形成导致活性丧失，但所得配合物的亲脂性和自由基清除能力与其杀锥虫作用相关。
