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首页> 外文期刊>Dalton transactions: An international journal of inorganic chemistry >New organoruthenium complexes with bioactive thiosemicarbazones as co-ligands: Potential anti-trypanosomal agents
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New organoruthenium complexes with bioactive thiosemicarbazones as co-ligands: Potential anti-trypanosomal agents

机译:具有生物活性的硫代半脲酮作为共配体的新型有机钌配合物:潜在的抗锥虫剂

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摘要

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.
机译:在寻找新的治疗工具来对抗锥虫病寄生虫所产生的被忽视的疾病,特别是针对非洲锥虫病(病原体为布鲁氏锥虫)的过程中,获得了有机钌化合物以及含有硫代半脲酮(L)作为配体的生物活性硝基呋喃。合成了四种通式为[Ru _2(p-cymeene)_2(L)_2] X _2的钌(ii)配合物,其中X = Cl或PF _6,并通过X射线解析了其中的两个晶体结构衍射法。这些复合物中的两种显示出对布鲁氏锥虫的显着体外生长抑制活性,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。这些令人鼓舞的结果使标题的有机钌化合物成为潜在抗胰锥管有机金属药物进一步发展的良好候选者。

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