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 e 0.22 mg/kg), and low toxicity in mice infected by Plasmodium vinckei.