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J Med Chem. 2005 May 19;48(10):3639-43.

Mono- and bis-thiazolium salts have potent antimalarial activity.

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  • 1Laboratoire des Amino acides Peptides et Protéines (LAPP) CNRS-UMR 5810, CP 19, Université Montpellier I, Place E. Bataillon, 34095 Montpellier Cedex 5, France.

Abstract

Three new series comprising 24 novel cationic choline analogues and consisting of mono- or bis (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 IC(50) values of 2.25 nM and 0.65 nM, respectively, against P. falciparum in vitro. These compounds also demonstrated good in vivo activity (ED(50) </= 0.22 mg/kg), and low toxicity in mice infected by Plasmodium vinckei.

[PubMed - indexed for MEDLINE]
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