3-Halo Chloroquine Derivatives Overcome Plasmodium falciparum Chloroquine Resistance Transporter-Mediated Drug Resistance in P. falciparum

被引：6

作者：

Edaye, Sonia ^{[1
]}

Tazoo, Dagobert ^{[2
]}

Bohle, D. Scott ^{[2
]}

Georges, Elias ^{[1
]}

机构：

[1] McGill Univ, Inst Parasitol, Ste Anne De Bellevue, PQ, Canada

[2] McGill Univ, Dept Chem, Montreal, PQ, Canada

来源：

ANTIMICROBIAL AGENTS AND CHEMOTHERAPY | 2015年 / 59卷 / 12期

基金：

加拿大自然科学与工程研究理事会;

关键词：

IN-VIVO; PRIMAQUINE; REVERSAL;

D O I：

10.1128/AAC.01139-15

中图分类号：

Q93 [微生物学];

学科分类号：

071005 ; 100705 ;

摘要：

Polymorphism in the Plasmodium falciparum chloroquine resistance transporter (PfCRT) was shown to cause chloroquine resistance. In this report, we examined the antimalarial potential of novel 3-halo chloroquine derivatives (3-chloro, 3-bromo, and 3-iodo) against chloroquine-susceptible and -resistant P. falciparum. All three derivatives inhibited the proliferation of P. falciparum; with 3-iodo chloroquine being most effective. Moreover, 3-iodo chloroquine was highly effective at potentiating and reversing chloroquine toxicity of drug-susceptible and -resistant P. falciparum.

引用

页码：7891 / 7893

页数：3

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