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N,O-螯合喹啉基半三明治型有机铑和铱配合物的合成、抗疟活性及作为 NAD 还原转移氢化催化剂的初步评价

N,O-Chelating quinoline-based half-sandwich organorhodium and -iridium complexes: synthesis, antiplasmodial activity and preliminary evaluation as transfer hydrogenation catalysts for the reduction of NAD.

机构信息

Department of Chemistry, University of Cape Town, Rondebosch, Cape Town, South Africa.

出版信息

Dalton Trans. 2019 Sep 21;48(35):13143-13148. doi: 10.1039/c9dt02030f. Epub 2019 Aug 16.

Abstract

Two Rh(iii) and Ir(iii) half-sandwich quinoline-based complexes were synthesised and evaluated for their in vitro antiplasmodial activity against the chloroquine-sensitive NF54 and multi-drug resistant K1 strains of the human malaria parasite, Plasmodium falciparum. These half-sandwich organometallic complexes can also facilitate transfer hydrogenation, by converting β-nicotinamide adenine dinucleotide (NAD) to its reduced form (NADH) in the presence of sodium formate. Co-administration of the iridium(iii) complex with sodium formate enhances the antiplasmodial activity in the chloroquine-resistant (K1) strain of Plasmodium falciparum, intimating that metal-mediated transfer hydrogenations can be achieved in malarial parasitic cells.

摘要

两种 Rh(iii) 和 Ir(iii) 半夹心喹啉基配合物被合成,并评估其对氯喹敏感的 NF54 和多药耐药的 K1 株人类疟原虫,恶性疟原虫的体外抗疟活性。这些半夹心金属有机配合物还可以通过在甲酸钠存在下将 β-烟酰胺腺嘌呤二核苷酸(NAD)转化为其还原形式(NADH)来促进转移氢化。铱(iii)配合物与甲酸钠联合给药可增强氯喹抗性(K1)株恶性疟原虫的抗疟活性,表明金属介导的转移氢化可以在疟原虫寄生细胞中实现。

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