Easily synthesized antimalarial ferrocene triazacyclononane quinoline conjugates

被引:53
作者
Biot, C
Dessolin, J
Ricard, I
Dive, D
机构
[1] Univ Lille 2, CNRS, Inst Biol, UMR 8525, F-59021 Lille, France
[2] Univ Lille 2, Inst Pasteur, F-59021 Lille, France
[3] Free Univ Brussels, B-1050 Brussels, Belgium
[4] Inst Europeen Chim & Biol, CNRS, UMR 5144, F-33607 Pessac, France
[5] Inst Pasteur, INSERM, U 547, F-59019 Lille, France
关键词
bioorganometallics; ferroquine; triazacyclononane; malaria; Plasmodium falciparum;
D O I
10.1016/j.jorganchem.2004.04.036
中图分类号
O61 [无机化学];
学科分类号
070301 ; 081704 ;
摘要
Starting from triazacyclononane, easily accessible ferrocenic quinoline derivatives were synthesized. Their antiplasmodial properties were investigated against chloroquine sensitive (HB3) and chloroquine-resistant (Dd2) Plasmodium falciparum. One of them, 7-chloro-4-[4-(7-chloro-4-quinolyl)-7-ferrocenylmethyl-1,4,7-triazacyclononan-1-yl]quinoline (4) showed potent antimalarial activity in vitro against the chloroquine-resistant strain Dd2 and therefore revealed to be the most promising lead from the present work for new organometallic antimalarial agents. (C) 2004 Elsevier B.V. All rights reserved.
引用
收藏
页码:4678 / 4682
页数:5
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