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首页> 外文期刊>Journal of biological inorganic chemistry: JBIC: a publication of the Society of Biological Inorganic Chemistry >Bioorganometallic chemistry-Evaluation of novel ruthenium(II)- and rhodium(III)- organosilane thiosemicarbazone complexes as antiparasitic agents
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Bioorganometallic chemistry-Evaluation of novel ruthenium(II)- and rhodium(III)- organosilane thiosemicarbazone complexes as antiparasitic agents

机译：生物有机金属化学-新型钌（II）-和铑（III）-有机硅烷硫代半碳杂complex配合物作为抗寄生虫剂的评估

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摘要

Parasitic diseases are rife in developing regions where the climate provides suitable conditions for replication and transmission. Malaria (an infectious disease) and trichomoniasis (a common STD) have become problematic due to the emergence of treatment-resistant strains.[1,2] Metals are recognised for their medicinal properties and have been introduced into organic systems with the idea that they may either aid with transportation into, or accumulation of the compound within, the active site. Metal ions allow for the addition of ancillary ligands which may lend properties such as lipophilicity or hydrophilicity to the complex as a whole. Therefore, the promising effects displayed by metal complexes in the treatment of parasitic diseases [e.g. Ferroquine (malaria)] motivated research into designing other metal-containing systems as potential treatments. Thiosemicarbazones (TSC's), known for a range of pharmacological properties (e.g. antiparasitic), are metal chelating ligands that have been studied in our group [3]. Organosilane compounds are also of interest as they generally exhibit enhanced pharmacological activity when compared with their non-silicon counterparts [4]. Therefore, in this study TSC's were combined with an organosilane moiety to explore compounds with increased potency and decreased susceptibility to resistant strains. In this presentation, the synthesis of organosilane TSC's and their complexes will be discussed, as well as their evaluation against plasmodium falciparum and trichomonas vaginalis.
机译：寄生虫病在发展中地区盛行，那里的气候为复制和传播提供了合适的条件。由于抗药性菌株的出现，疟疾（一种传染病）和滴虫病（一种常见的性病）已成为问题。[1,2]金属以其药用特性而闻名，并已被引入有机体系，其想法是可能有助于将化合物运输到活性部位或在活性部位内积累。金属离子允许添加辅助配体，其可以给整个复合物带来诸如亲脂性或亲水性的性质。因此，金属络合物在治疗寄生虫病方面显示出令人鼓舞的效果[例如， [Ferroquine（疟疾）]促使人们进行研究，以设计其他含金属的系统作为潜在的治疗方法。硫代氨基咔唑（TSC's）以其一系列的药理特性（例如抗寄生虫药）而闻名，是我们小组中已研究的金属螯合配体[3]。有机硅烷化合物也是令人感兴趣的，因为与非硅化合物相比，它们通常表现出增强的药理活性[4]。因此，在这项研究中，将TSC与有机硅烷部分结合使用，以探索具有更高效价和对耐药菌株敏感性降低的化合物。在本演讲中，将讨论有机硅烷TSC及其配合物的合成，以及它们对恶性疟原虫和阴道毛滴虫的评估。

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