Application of multicomponent reactions to antimalarial drug discovery. Part 3: Discovery of aminoxazole 4-aminoquinolines with potent antiplasmodial activity in vitro

被引:37
|
作者
Musonda, Chitalu C.
Little, Susan
Yardley, Vanessa
Chibale, Kelly [1 ]
机构
[1] Univ Cape Town, Dept Chem, ZA-7701 Rondebosch, South Africa
[2] London Sch Hyg & Trop Med, Dept Infect & Trop Dis, London WC1E 7HT, England
[3] Univ Cape Town, Inst Infect Dis & Mol Med, ZA-7701 Rondebosch, South Africa
基金
新加坡国家研究基金会;
关键词
4-aminoquinolines; aminoxazoles; malaria; P; falciparum; antiplasmodial activity;
D O I
10.1016/j.bmcl.2007.06.070
中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
The synthesis and antimalarial activity of a novel series of first generation 4-aminoquinoline-containing 2,4,5-trisubstituted aminoxazoles against two strains of the Plasmodium falciparum parasite in vitro is described. A number of compounds significantly more potent than the standard drug chloroquine were identified. (c) 2007 Elsevier Ltd. All rights reserved.
引用
收藏
页码:4733 / 4736
页数:4
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