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首页> 外文期刊>Bioorganic and Medicinal Chemistry Letters >Synthesis, spectral studies and in vitro assessment for antiamoebic activity of new cyclooctadiene ruthenium(II) complexes with 5-nitrothiophene-2-carboxaldehyde thiosemicarbazones.
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Synthesis, spectral studies and in vitro assessment for antiamoebic activity of new cyclooctadiene ruthenium(II) complexes with 5-nitrothiophene-2-carboxaldehyde thiosemicarbazones.

机译:新型环辛二烯钌(II)与5-硝基噻吩-2-羧醛硫代半缩氮唑配合物的抗厌氧活性的合成,光谱研究和体外评估。

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摘要

We report here the synthesis, characterization and in vitro antiamoebic activity of 5-nitrothiophene-2-carboxaldehyde thiosemicarbazones (TSC), 1-5, and their bidentate complexes [Ru(eta(4)-C(8)H(12))(TSC)Cl(2)] 1a-5a. The biological studies of these compounds were investigated against HK-9 strain of Entamoeba histolytica and the concentration causing 50% cell growth inhibition (IC(50)) was calculated in the micromolar range. The ligands exhibited antiamoebic activity in the range (2.05-5.29microM). Screening results indicated that the potencies of the compounds increased by the incorporation of ruthenium(II) in the thiosemicarbazones. The complexes 1a-5a showed antiamoebic activity with an IC(50) of 0.61-1.43microM and were better inhibitors of growth of E. histolytica, based on IC(50) values. The most promising among them is Ru(II) complex 2a having 1,2,3,4-tetrahydroquinoline as N(4) substitution.
机译:我们在这里报告的合成,表征和5-硝基噻吩-2-羧甲醛硫代半脲酮(TSC),1-5和其双齿络合物[Ru(eta(4)-C(8)H(12))的体外抗厌氧活性(TSC)Cl(2)] 1a-5a。对这些化合物针对溶血性变形杆菌的HK-9菌株进行了生物学研究,并计算了在微摩尔范围内引起50%细胞生长抑制的浓度(IC(50))。所述配体显示出在(2.05-5.29microM)范围内的抗厌氧活性。筛选结果表明,通过将钌(II)掺入到硫代半脲酮中,化合物的效力得以提高。配合物1a-5a表现出抗氧活性,IC(50)为0.61-1.43microM,基于IC(50)值,它是溶血性大肠杆菌的更好的抑制剂。其中最有希望的是具有1,2,3,4-四氢喹啉作为N(4)取代的Ru(II)络合物2a。

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