Pentamethylcyclopentadienyl-rhodium and iridium complexes containing (N^N and N^O) bound chloroquine analogue ligands: synthesis, characterization and antimalarial properties.
Pentamethylcyclopentadienyl-rhodium and iridium complexes containing (N^N and N^O) bound chloroquine analogue ligands: synthesis, characterization and antimalarial properties.
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含有（N^N 和 N^O）结合氯喹类似物配体的五甲基环戊二烯基铑和铱络合物：合成、表征和抗疟特性。
DOI：
10.1039/c5dt03739e
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发表时间：
2016
影响因子：
4
通讯作者：
E. Nordlander
中科院分区：
文献类型：
--
作者：
Erik Ekengard;Kamlesh Kumar;Thibault Fogeron;C. de Kock;Peter J. Smith;M. Haukka;M. Monari;E. Nordlander
描述了含有 N^N 和 N^O-螯合氯喹类似物配体的 20 种新型五甲基环戊二烯基铑和铱配合物的合成和表征。针对氯喹敏感 (CQS) NF54 和氯喹抗性 (CQR) Dd2 恶性疟原虫菌株，评估了新配体以及复合物的体外抗疟活性。发现抗疟活性为良好至中等；尽管所有配合物的活性均低于青蒿琥酯，但某些配体和配合物显示出比氯喹（CQ）更好的活性。特别是，发现铑配合物对 CQS NF54 菌株的活性比铱配合物高得多。在水杨基部分的对位具有吸电子基团（F、Cl、Br、I和NO2）的水杨醛亚胺席夫碱配体及其铑配合物对CQS-NF54和CQR-Dd2菌株均表现出良好的抗疟原虫活性。 (η(5)-五甲基环戊二烯基){N(1)-(7-氯喹啉-4-基)-N(2)-(吡啶-2-基甲基)乙烷-1,2-二胺)}氯化氯化铑(III)和的晶体结构报道了(η(5)-五甲基环戊二烯基){(4-氯-2-(((2-((7-氯喹啉-4-基)氨基)乙基)亚氨基)甲基)苯酚盐)}氯铑(III)氯化物。氨基-吡啶基配合物 (η(5)-五甲基环戊二烯基){(N(1)-(7-氯喹啉-4-基)-N(2)-(吡啶-2-基甲基)乙烷-1,2-二胺)}氯化氯化铱(III)在丙酮中的结晶导致亚氨基-吡啶基衍生物的形成(η(5)-五甲基环戊二烯基){(N1-(7-氯喹啉-4-基)-N2-(吡啶-2-基亚甲基)乙烷-1,2-二胺)}氯化氯化铱(III)，还报道了其晶体结构。
The synthesis and characterization of twenty new pentamethylcyclopentadienyl-rhodium and iridium complexes containing N^N and N^O-chelating chloroquine analogue ligands are described. The in vitro antimalarial activity of the new ligands as well as the complexes was evaluated against the chloroquine sensitive (CQS) NF54 and the chloroquine resistant (CQR) Dd2 strains of Plasmodium falciparum. The antimalarial activity was found to be good to moderate; although all complexes are less active than artesunate, some of the ligands and complexes showed better activity than chloroquine (CQ). In particular, rhodium complexes were found to be considerably more active than iridium complexes against the CQS NF54 strain. Salicylaldimine Schiff base ligands having electron-withdrawing groups (F, Cl, Br, I and NO2) in para position of the salicyl moiety and their rhodium complexes showed good antiplasmodial activity against both the CQS-NF54 and the CQR-Dd2 strains. The crystal structures of (η(5)-pentamethylcyclopentadienyl){N(1)-(7-chloroquinolin-4-yl)-N(2)-(pyridin-2-ylmethyl)ethane-1,2-diamine)} chlororhodium(III) chloride and (η(5)-pentamethylcyclopentadienyl){(4-chloro-2-(((2-((7-chloroquinolin-4-yl)amino)ethyl)imino)methyl)phenolate)}chlororhodium(III) chloride are reported. The crystallization of the amino-pyridyl complex (η(5)-pentamethylcyclopentadienyl){(N(1)-(7-chloroquinolin-4-yl)-N(2)-(pyridin-2-ylmethyl)ethane-1,2-diamine)}chloroiridium(III) chloride in acetone resulted in the formation of the imino-pyridyl derivative (η(5)-pentamethylcyclopentadienyl){(N1-(7-chloroquinolin-4-yl)-N2-(pyridin-2-ylmethylene)ethane-1,2-diamine)}chloroiridium(III) chloride, the crystal structure of which is also reported.
影响因子：
2.9
作者：
Leed, A;DuBay, K;Roepe, PD
通讯作者：
Roepe, PD