Cátedra de Química Inorgánica, Departamento Estrella Campos, Facultad de Química, Universidad de la República (UdelaR), Gral. Flores 2124, 11800, Montevideo, Uruguay.
Dalton Trans. 2012 Feb 7;41(5):1534-43. doi: 10.1039/c1dt11519g. Epub 2011 Dec 2.
In the search for new therapeutic tools against neglected diseases produced by trypanosomatid parasites, and particularly against African Trypanosomiasis, whose etiological agent is Trypanosoma brucei, organoruthenium compounds with bioactive nitrofuran containing thiosemicarbazones (L) as co-ligands were obtained. Four ruthenium(II) complexes with the formula [Ru(2)(p-cymene)(2)(L)(2)]X(2), where X = Cl or PF(6), were synthesized and the crystal structures of two of them were solved by X-ray diffraction methods. Two of the complexes show significant in vitro growth inhibition activity against Trypanosoma brucei brucei and are highly selective towards trypanosomal cells with respect to mammalian cells (J774 murine macrophages). These promising results make the title organoruthenium compounds good lead candidates for further developments towards potential antitrypanosomal organometallic drugs.
在寻找针对由利什曼原虫寄生虫引起的被忽视疾病的新治疗工具,特别是针对其病原体为布氏锥虫的非洲锥虫病方面,获得了含有生物活性硝呋咱的含硫代半卡巴腙(L)的有机钌化合物作为共配体。合成了四个具有化学式[Ru(2)(p-cymene)(2)(L)(2)]X(2)的钌(II)配合物,其中 X = Cl 或 PF(6),并通过 X 射线衍射方法解决了其中两个的晶体结构。其中两个配合物对布氏锥虫布鲁斯氏亚种表现出显著的体外生长抑制活性,并且相对于哺乳动物细胞(J774 鼠巨噬细胞)对锥虫细胞具有高度选择性。这些有希望的结果使得标题有机钌化合物成为进一步开发潜在抗锥虫金属有机药物的良好先导候选物。