Mono- and bis-thiazolium salts have potent antimalarial activity

被引：73
|
作者：
Hamzé, A
Rubi, E
Arnal, P
Boisbrun, M
Carcel, C
Salom-Roig, X
Maynadier, M
Wein, S
Vial, H
Calas, M
机构：
[1] Univ Montpellier 1, Lab Amino Acides Peptides & Prot, CNRS, UMR 5810, F-34095 Montpellier, France
[2] Univ Montpellier 2, CNRS, UMR 5539, DMIM, F-34095 Montpellier, France
来源：
JOURNAL OF MEDICINAL CHEMISTRY | 2005年 / 48卷 / 10期
关键词：
D O I：
10.1021/jm0492608
中图分类号：
R914 [药物化学];
学科分类号：
100701 ;
摘要：
Three new series comprising 24 novel cationic choline analogues and consisting of mono- or his (N or C-5-duplicated) thiazolium salts have been synthesized. Bis-thiazolium salts showed potent antimalarial activity (much superior to monothiazoliums). Among them, bis-thiazolium salts 12 and 13 exhibited IC50 values of 2.25 nM and 0.65 nM, respectively, against P. falciparum in vitro. These compounds also demonstrated good in vivo activity (ED50 <= 0.22 mg/kg), and low toxicity in mice infected by Plasmodium vinckei.
引用
收藏
页码：3639 / 3643
页数：5
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