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首页> 外文期刊>Dalton transactions: An international journal of inorganic chemistry >Bioisosteric ferrocenyl-containing quinolines with antiplasmodial and antitrichomonal properties
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Bioisosteric ferrocenyl-containing quinolines with antiplasmodial and antitrichomonal properties

机译：具有抗血浆和抗毛滴虫特性的生物甾族二茂铁基喹啉

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摘要

Bioisosteric ferrocenyl-containing quinolines and ferrocenylamines containing organosilanes and their carbon analogues, were prepared and fully characterised. The molecular structures of two ferrocenylcontaining quinolines, determined using single-crystal X-ray diffraction, revealed that the compounds crystallise in a folded conformation. The compounds were screened for their antiplasmodial activity against the chloroquine-sensitive (NF54) and CQ-resistant (Dd2) strains of P. falciparum, as well as for their cytotoxicity against Chinese Hamster Ovarian (CHO) cells. The ferrocenyl-containing quinolines displayed activities in the low nanomolar range (6-36 nM), and showed selectivity towards parasites. p-Haematin inhibition assays suggest that the compounds may in part act via the inhibition of haemozoin formation, while microsomal metabolic stability studies reveal that the ferrocenyl-containing quinolines are rapidly metabolised in liver microsomes. Further, antitrichomonal screening against the metronidazole-sensitive (G3) strain of the mucosal pathogen T vaginalis revealed that the quinoline-based compounds displayed superior parasite growth inhibition when compared to the ferrocenylamines. The library was also tested E. coil and on Lactobacilli spp. found as part of the normal flora of the human microbiome and no effect on growth in vitro was observed, supporting the observation that these compounds are specific for eukaryotic pathogens.
机译：制备并充分表征了生物立体异构的含二茂铁基的喹啉和含二茂铁基胺的有机硅烷及其碳类似物。使用单晶X射线衍射测定的两个含二茂铁基喹啉的分子结构表明，这些化合物以折叠构型结晶。筛选了这些化合物对恶性疟原虫的氯喹敏感（NF54）和耐CQ（Dd2）菌株的抗疟原虫活性，以及​​对中国仓鼠卵巢（CHO）细胞的细胞毒性。含二茂铁基的喹啉在低纳摩尔范围（6-36 nM）内显示活性，并显示出对寄生虫的选择性。 p-Haematin抑制试验表明，这些化合物可能部分通过抑制血红素形成而起作用，而微粒体代谢稳定性研究表明，含二茂铁基的喹啉在肝微粒体中迅速代谢。此外，针对甲硝唑敏感性（G3）的粘膜病原体T阴道菌的抗滴虫筛选显示，与二茂铁基胺相比，基于喹啉的化合物显示出优异的寄生虫生长抑制作用。还对该文库进行了大肠杆菌和乳杆菌属的测试。被发现是人类微生物组正常菌群的一部分，并且未观察到对体外生长的影响，支持了这些化合物对真核病原体具有特异性的观察。

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