Fluorene-Chloroquine Hybrids: Synthesis, in vitro Antiplasmodial Activity, and Inhibition of Heme Detoxification Machinery of Plasmodium falciparum,ChemMedChem

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Fluorene-Chloroquine Hybrids: Synthesis, in vitro Antiplasmodial Activity, and Inhibition of Heme Detoxification Machinery of Plasmodium falciparum
ChemMedChem ( IF 3.6 ) Pub Date : 2022-08-26 , DOI: 10.1002/cmdc.202200414
Parth ₁ , Navpreet Kaur ₂ , Constance Korkor ₃ , Shaikh M Mobin _{2,

4,

5} , Kelly Chibale ₃ , Kamaljit Singh ₁

Affiliation

Malaria detox: Fluorene-chloroquine hybrids represent a new class of highly active antiplasmodial agents. The most active compound shows high in vitro antiplasmodial activity (IC₅₀=139 nM) against a chloroquine-sensitive NF54 strain of the human malaria parasite Plasmodium falciparum. The hybrid binds to hemin and inhibits β-hematin formation and impacts the detoxification machinery in P. falciparum.

中文翻译：

芴-氯喹杂化物：合成、体外抗疟原虫活性和对恶性疟原虫血红素解毒机制的抑制

疟疾排毒：芴-氯喹杂化物代表了一类新型的高效抗疟原虫药物。活性最强的化合物对人类疟疾寄生虫恶性疟原虫的氯喹敏感 NF54 菌株显示出高体外抗疟原虫活性 (IC ₅₀ =139 nM) 。该杂合体与血红素结合并抑制 β-血红素的形成，并影响恶性疟原虫的解毒机制。

更新日期：2022-08-26

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