Antiplasmodial activity of a series of 1,3,5-triazine-substituted polyamines

被引:31
作者
Klenke, B
Barrett, MP
Brun, R
Gilbert, IH
机构
[1] Cardiff Univ, Welsh Sch Pharm, Cardiff CF10 3XF, S Glam, Wales
[2] Univ Glasgow, Inst Biomed & Life Sci, Div Infect & Immun, Glasgow G12 8QQ, Lanark, Scotland
[3] Swiss Trop Inst, CH-4002 Basel, Switzerland
基金
英国惠康基金;
关键词
Plasmodium falciparum; malaria; parasites; protozoa; polyamine metabolism;
D O I
10.1093/jac/dkg307
中图分类号
R51 [传染病];
学科分类号
100401 ;
摘要
Polyamine biosynthesis and function has been shown to be a good drug target in some parasitic protozoa and it is proposed that the pathway might also represent a target in the malaria parasite Plasmodium falciparum. A series of 1,3,5-triazine-substituted polyamine analogues were tested for activity against Plasmodium falciparum in vitro. The series showed activity against the parasites and were generally more active against the chloroquine-resistant line K1 than the chloroquine-susceptible line NF54. Simple unbranched analogues had better activity than analogues carrying branched or cyclic central chains. Addition of multiple triazine units in general led to increased activity of the compounds.
引用
收藏
页码:290 / 293
页数:4
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