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首页> 外文期刊>Dalton transactions: An international journal of inorganic chemistry >Improved antiparasitic activity by incorporation of organosilane entities into half-sandwich ruthenium(II) and rhodium(III) thiosemicarbazone complexes
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Improved antiparasitic activity by incorporation of organosilane entities into half-sandwich ruthenium(II) and rhodium(III) thiosemicarbazone complexes

机译：通过将有机硅烷实体掺入半夹心钌（II）和铑（III）硫代半脲配合物中来提高抗寄生虫活性

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摘要

A series of ferrocenyl- and aryl-functionalised organosilane thiosemicarbazone compounds was obtained via a nucleophilic substitution reaction with an amine-terminated organosilane. The thiosemicarbazone (TSC) ligands were further reacted with either a ruthenium dimer [(eta(6)-(PrC6H4Me)-Pr-i)Ru(mu-Cl)Cl](2) or a rhodium dimer [(Cp*)-Rh(mu-Cl)Cl](2) to yield a series of cationic mono- and binuclear complexes. The thiosemicarbazone ligands, as well as their metal complexes, were characterised using NMR and IR spectroscopy, and mass spectrometry. The molecular structure of the binuclear ruthenium(II) complex was determined by single-crystal X-ray diffraction analysis. The thiosemicarbazones and their complexes were evaluated for their in vitro antiplasmodial activities against the chloroquine-sensitive (NF54) and chloroquine-resistant (Dd2) Plasmodium falciparum strains, displaying activities in the low micromolar range. Selected compounds were screened for potential beta-haematin inhibition activity, and it was found that two Rh(III) complexes exhibited moderate to good inhibition. Furthermore, the compounds were screened for their antitrichomonal activities against the G3 Trichomonas vaginalis strain, revealing a higher percentage of growth inhibition for the ruthenium and rhodium complexes over their corresponding ligand.
机译：通过与胺封端的有机硅烷的亲核取代反应，获得了一系列二茂铁基和芳基官能化的有机硅烷硫半碳carb化合物。硫半脲酮（TSC）配体进一步与钌二聚体[（eta（6）-（PrC6H4Me）-Pr-1）Ru（mu-Cl）Cl]（2）或铑二聚体[（Cp *）- Rh（mu-Cl）Cl]（2）产生一系列阳离子单核和双核配合物。使用NMR和IR光谱，以及质谱法对thiosemicarbazone配体及其金属配合物进行表征。双核钌（II）配合物的分子结构通过单晶X射线衍射分析确定。评估了硫代半氨基甲酮及其配合物对恶性疟原虫对氯喹敏感（NF54）和耐氯喹（Dd2）的体外抗疟原虫活性，显示了在低微摩尔范围内的活性。对选定的化合物筛选潜在的β-血红素抑制活性，发现两种Rh（III）配合物表现出中等至良好的抑制作用。此外，针对所述化合物筛选了针对G3阴道滴虫的抗滴虫活性，显示出相对于其配体而言，钌和铑配合物具有更高的生长抑制百分比。

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