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首页> 外文期刊>Dalton transactions: An international journal of inorganic chemistry >Antimalarial activity of ruthenium(II) and osmium(II) arene complexes with mono- and bidentate chloroquine analogue ligands
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Antimalarial activity of ruthenium(II) and osmium(II) arene complexes with mono- and bidentate chloroquine analogue ligands

机译：具有单和双齿氯喹类似物配体的钌（II）和（II）芳烃配合物的抗疟活性

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摘要

Eight new ruthenium and five new osmium p-cymene half-sandwich complexes have been synthesized, characterized and evaluated for antimalarial activity. All complexes contain ligands that are based on a 4-chloroquinoline framework related to the antimalarial drug chloroquine. Ligands HL1-8 are salicylaldimine derivatives, where HL1 = N-(2-((2-hydroxyphenyl)methylimino)ethyl)-7-chloroquinolin-4-amine, and HL2-8 contain non-hydrogen substituents in the 3-position of the salicylaldimine ring, viz. F, Cl, Br, I, NO2, OMe and Bu-t for HL2-8, respectively. Ligand HL9 is also a salicylaldimine-containing ligand with substitutions in both 3- and 5-positions of the salicylaldimine moiety, i.e. N-(2-((2-hydroxy-3,5-di-tert-butylphenyl) methyl-imino)ethyl)-7-chloroquinolin-4-amine, while HL10 is N-(2-((1-methyl-1H-imidazol-2-yl)-methylamino)ethyl)-7-chloroquinolin-4-amine) The half sandwich metal complexes that have been investigated are [Ru(eta(6)-cym)(L1-8)Cl] (Ru-1-Ru-8, cym = p-cymene), [Os(eta(6)-cym)(L-1-3,L-5,L-7)Cl] (Os-1-Os-3, Os-5, and Os-7), [M(eta(6)-cym)(HL9)Cl-2] (M = Ru, Ru-HL9; M = Os, Os-HL9) and [M(eta(6)-cym)(L-10)Cl]Cl (M = Ru, Ru-10; M = Os, Os-10). In complexes Ru-1-Ru-8 and Ru-10, Os-1-Os-3, Os-5 and Os-7 and Os-10, the ligands were found to coordinate as bidentate N,O- and N,N-chelates, while in complexes Ru-HL9 and Os-HL9, monodentate coordination of the ligands through the quinoline nitrogen was established. The antimalarial activity of the new ligands and complexes was evaluated against chloroquine sensitive (NF54 and D10) and chloroquine resistant (Dd2) Plasmodium falciparum malaria parasite strains. Coordination of ruthenium and osmium arene moieties to the ligands resulted in lower antiplasmodial activities relative to the free ligands, but the resistance index is better for the ruthenium complexes compared to chloroquine. Overall, osmium complexes appeared to be less active than the corresponding ruthenium complexes.
机译：合成了八种新的钌和五种新的对-cy烯半夹心复合物，表征并评估了其抗疟活性。所有复合物均包含基于与抗疟疾药物氯喹有关的4-氯喹啉骨架的配体。配体HL1-8是水杨醛亚胺衍生物，其中HL1 = N-（2-（（（2-羟苯基）甲基亚氨基）乙基）-7-氯喹啉-4-胺，HL2-8在其3位上含有非氢取代基水杨醛亚胺环，即。 HL2-8的F，Cl，Br，I，NO2，OMe和Bu-t。配体HL9还是含水杨醛亚胺的配体，在水杨醛亚胺部分的3-和5-位均具有取代基，即N-（2-（（2-羟基-3,5-二叔丁基苯基）甲基-亚氨基）乙基）-7-氯喹啉-4-胺，而HL10是N-（2-（（1-甲基-1H-咪唑-2-基）-甲基氨基）乙基）-7-氯喹啉-4-胺）已研究的金属络合物为[Ru（eta（6）-cym）（L1-8）Cl]（Ru-1-Ru-8，cym = p-cymene），[Os（eta（6）-cym） （L-1-3，L-5，L-7）Cl]（Os-1-Os-3，Os-5和Os-7），[M（eta（6）-cym）（HL9）Cl -2]（M = Ru，Ru-HL9; M = Os，Os-HL9）和[M（eta（6）-cym）（L-10）Cl] Cl（M = Ru，Ru-10; M = Os，Os-10）。在配合物Ru-1-Ru-8和Ru-10，Os-1-Os-3，Os-5和Os-7和Os-10中，发现配体以N，O-和N，N为二齿配位-螯合物，而在复合物Ru-HL9和Os-HL9中，通过喹啉氮建立了配体的单齿配位。评估了新配体和复合物的抗疟活性，它们对氯喹敏感（NF54和D10）和对氯喹具有抵抗力（Dd2）的恶性疟原虫疟原虫菌株。钌和芳烃部分与配体的配位导致相对于游离配体较低的抗疟原虫活性，但是与氯喹相比，钌配合物的抗性指数更好。总体而言，络合物的活性似乎不如相应的钌络合物。

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