首页> 外文期刊>European Journal of Medicinal Chemistry: Chimie Therapeutique >New Pd(II) complexes of the synthesized 1-N-substituted thiosemicarbazones of 3-indole carboxaldehyde: characterization and antiamoebic assessment against E. histolytica.
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New Pd(II) complexes of the synthesized 1-N-substituted thiosemicarbazones of 3-indole carboxaldehyde: characterization and antiamoebic assessment against E. histolytica.

机译:合成的3-吲哚甲醛的1-N-取代硫代半脲的新Pd(II)配合物:针对溶组织性大肠杆菌的表征和抗厌氧性评估。

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摘要

Reaction of 3-indole carboxaldehyde with aminothiocarbonyl hydrazines resulted in the formation of 3-indole carboxaldehyde thiosemicarbazones (TSCs) 1-13. The synthesized thiosemicarbazones were used as ligands in the formation of [Pd(TSC)Cl2] complexes with palladium(II) metal ion precursor, [Pd(DMSO)2Cl2]. The chemical structures of all the compounds were established by electronic, IR, 1H NMR and 13C NMR spectral data. The structure of the complexes was further established by FABMS and DTA. It is concluded that the thione sulphur and the azomethine nitrogen atom of the ligands are bonded to the metal ion. The testing of the antiamoebic activity of these compounds against the protozoan parasite Entamoeba histolytica suggests that compounds 5, 3a, 5a and 8a-13a might be endowed with important antiamoebic properties since they showed less IC50 values than metronidazole. Moreover, compound 12a displays remarkable antiamoebic activity than metronidazole (IC50 values of 0.29 vs 1.81 microM, respectively). MTT assay showed that the compounds are non-toxic to human kidney epithelial cell line.
机译:3-吲哚羧醛与氨基硫代羰基肼的反应导致形成3-吲哚羧醛硫代半咔唑(TSC)1-13。合成的硫代半氨基甲酮用作配体,与钯(II)金属离子前体[Pd(DMSO)2Cl2]形成[Pd(TSC)Cl2]配合物。通过电子,IR,1H NMR和13C NMR光谱数据确定所有化合物的化学结构。 FABMS和DTA进一步建立了复合物的结构。结论是,配体的硫酮硫和偶氮甲碱氮原子与金属离子键合。对这些化合物对原生动物寄生虫组织解脂Entamoeba histolytica的抗厌氧活性测试表明,化合物5、3a,5a和8a-13a可能具有重要的抗厌氧性能,因为它们的IC50值低于甲硝唑。此外,化合物12a显示出比甲硝唑显着的抗厌氧活性(IC50值分别为0.29对1.81 microM)。 MTT测定表明该化合物对人肾上皮细胞系无毒。

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