Synthesis and in vitro and in vivo antimalarial activity of new 4-anilinoquinolines

被引：51

作者：

Delarue, S

Girault, S

Maes, L

Debreu-Fontaine, MA

Labaeïd, M

Grellier, P

Sergheraert, C

机构：

[1] Univ Lille 2, UMR CNRS 8525, Inst Biol, F-59021 Lille, France

[2] Univ Lille 2, UMR CNRS 8525, Inst Pasteur, F-59021 Lille, France

[3] Museum Natl Hist Nat, IFR CNRS 63, Lab Biol Parasitaire, F-75005 Paris, France

[4] Tibotec, B-32800 Mechelen, Belgium

来源：

JOURNAL OF MEDICINAL CHEMISTRY | 2001年 / 44卷 / 17期

关键词：

D O I：

10.1021/jm010842o

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

A new series of 4-anilinoquinolines with two proton-accepting side chains has been synthesized. Antimalarial activity and levels of cytotoxicity upon both MRC-5 cells and macrophages were found to be highly dependent upon the features of these side chains. Several compounds were found to be active in the low nanomolar range, against both chloroquine-sensitive and -resistant strains of Plasmodium falciparum in vitro. From among them, a morpholino derivative cured mice infected by Plasmodium berghei and displayed a lower toxicity than amodiaquine upon mouse macrophages.

引用

页码：2827 / 2833

页数：7

共 31 条

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