Synthesis and in vitro and in vivo antimalarial activity of N1-(7-chloro-4-quinolyl)-1,4-bis(3-aminopropyl)piperazine derivatives

被引：115

作者：

Ryckebusch, A

Deprez-Poulain, R

Maes, L

Debreu-Fontaine, MA

Mouray, E

Grellier, P

Sergheraert, C

机构：

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

[2] Inst Pasteur, F-59021 Lille, France

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

[4] Tibotec, B-32800 Mechelen, Belgium

来源：

JOURNAL OF MEDICINAL CHEMISTRY | 2003年 / 46卷 / 04期

关键词：

D O I：

10.1021/jm020960r

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

Three series of monoquinolines consisting of a 1,4-bis(3-aminopropyl)piperazine linker and a large variety of terminal groups were synthesized. Our aim was to prove that in related bisquinoline, it is the second quinoline moiety that is responsible for cytotoxicity and that it is not an absolute requirement for overcoming resistance to chloroquine (CQ). Eleven compounds displayed a higher selectivity index (ratio CC50/IC50 activity) than CQ and one of them cured mice infected by Plasmodium berghei.

引用

页码：542 / 557

页数：16

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