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

页码：3639 / 3643

页数：5

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