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首页> 外文期刊>Dalton transactions: An international journal of inorganic chemistry >Synthesis, characterisation and antitubercular activities of a series of pyruvate-containing aroylhydrazones and their Cu-complexes
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Synthesis, characterisation and antitubercular activities of a series of pyruvate-containing aroylhydrazones and their Cu-complexes

机译：一系列含丙酮酸的芳酰hydr及其铜配合物的合成，表征和抗结核活性

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摘要

A series of eight pyruvate-based aroylhydrazones was synthesised and characterised. The reaction of the sodium salts of the aroylhydrazones with one equivalent of copper(ii) chloride allowed the isolation of neutral 1:1 complexes in which the hydrazones occupy three basal coordination sites of a square pyramidal Cu(ii)-centre, with two solvent molecules completing the coordination sphere. Structural details were obtained through the determination of the crystal structures of two representative pyruvate-based aroylhydrazones and three Cu(ii) complexes. The evaluation of the antimycobacterial activity of the sodium salts of the eight pryruvate hydrazones showed that the compounds are essentially inactive in their anionic form. The corresponding neutral Cu(ii) complexes, however, exhibit promising antimycobacterial activities if tested under high iron (8 μg Fe per mL) conditions. As observed for the related antimycobacterial agent isoniazid, the activity of the complexes decreases if the M. tuberculosis cells are grown under low iron (0.02 μg Fe per mL) conditions. The Cu(ii) complexes may thus have a similar mode of action and may require an iron-containing heme-dependent peroxidase for activation. This journal is
机译：合成并表征了一系列八个基于丙酮酸酯的芳酰基yl。芳酰hydr的钠盐与一当量的氯化铜（ii）的反应可分离中性的1：1络合物，其中占据了方形金字塔形Cu（ii）中心的三个基本配位点，并带有两种溶剂分子完成协调领域。通过确定两个代表性的基于丙酮酸的芳酰hydr和三个Cu（ii）配合物的晶体结构，获得了结构细节。对八种丙酮酸的钠盐的抗分枝杆菌活性的评估表明，该化合物以其阴离子形式基本上是无活性的。但是，如果在高铁（每毫升8微克铁）条件下进行测试，相应的中性Cu（ii）配合物将显示出有希望的抗分枝杆菌活性。如对相关抗分枝杆菌药异烟肼所观察到的，如果结核分枝杆菌细胞在低铁（0.02微克铁/毫升）条件下生长，复合物的活性就会降低。因此，Cu（ii）配合物可能具有相似的作用方式，并可能需要含铁血红素依赖性过氧化物酶进行激活。这本日记是

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