首页> 外文期刊>European Journal of Medicinal Chemistry: Chimie Therapeutique >Synthesis, characterization and in vitro Antiamoebic Activity of 5-nitrothiophene-2-carboxaldehyde thiosemicarbazones and their Palladium (II) and Ruthenium (II) Complexes.
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Synthesis, characterization and in vitro Antiamoebic Activity of 5-nitrothiophene-2-carboxaldehyde thiosemicarbazones and their Palladium (II) and Ruthenium (II) Complexes.

机译:5-硝基噻吩-2-羧甲醛硫代半脲酮及其钯(II)和钌(II)配合物的合成,表征和体外抗厌氧活性。

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Synthesis of new Palladium(II) and Ruthenium(II) complexes of the type, [Pd(L)Cl(2)] and [Ru(eta(4)-C(8)H(12))(L)Cl(2)] {where, L = thiosemicarbazones derived from 5-nitrothiophene-2-carboxaldehyde and cycloalkylaminothiocarbonyl hydrazines} have been isolated by the reaction of [Pd(DMSO)(2)Cl(2)] and [Ru(eta(4)-C(8)H(12))(CH(3)CN)(2)Cl(2)] with 5-nitrothiophene-2-carboxaldehyde thiosemicarbazones. The spectral data revealed that the thiosemicarbazones act as bidentate ligands, making use of thionic sulphur and the azomethine nitrogen atom for coordination to the central metal ion. Microdilution method was used for the assessment of antiamoebic activity of all the compounds against HK-9 strain of Entamoeba histolytica. Among all the thiosemicarbazones, 5-NT-4-BPTSCN (3) showed significant antiamoebic activity (IC(50) - 2.56 microM). Enhancement of antiamoebic activity resulted by introducing palladium and ruthenium metals in the thiosemicarbazone moiety. All the Pd(II) and Ru(II) complexes of 5-nitrothiophene-2-carboxaldehyde thiosemicarbazones were found more active then their respective ligands. The complexes 1a-4a, 1b and 3b showed antiamoebic activity.
机译:新型[Pd(L)Cl(2)]和[Ru(eta(4)-C(8)H(12))(L)Cl()的新钯(II)和钌(II)配合物的合成2)] {其中,L =衍生自5-硝基噻吩-2-甲醛和环烷基氨基硫羰基肼的硫代半咔唑}已通过[Pd(DMSO)(2)Cl(2)]和[Ru(eta(4) -C(8)H(12))(CH(3)CN)(2)Cl(2)]与5-硝基噻吩-2-羧醛硫代半氨基甲酮光谱数据表明,硫代半氨基甲酮起着双齿配体的作用,它利用硫杂硫和甲亚胺氮原子与中心金属离子配位。微稀释法用于评估所有化合物对溶组织变形杆菌的HK-9菌株的抗厌氧活性。在所有的硫代半脲酮中,5-NT-4-BPTSCN(3)表现出显着的抗阿米巴活性(IC(50)-2.56 microM)。通过在硫半脲部分中引入钯和钌金属,可以增强抗厌氧活性。发现5-硝基噻吩-2-羧甲醛硫代半氨基甲酮的所有Pd(II)和Ru(II)配合物均比其各自的配体更具活性。配合物1a-4a,1b和3b显示出抗厌氧活性。

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