[EN] PYRIMIDINE COMPOUND, PHARMACEUTICAL COMPOSITION COMPRISING SAME, PREPARATION METHOD THEREFOR, AND USE THEREOF<br/>[FR] COMPOSÉ PYRIMIDINE, COMPOSITION PHARMACEUTIQUE LE COMPRENANT, SON PROCÉDÉ DE PRÉPARATION ET SON UTILISATION<br/>[ZH] 嘧啶类化合物、包含其的药物组合物、其制备方法及其用途
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.
DE675617
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Clarke; Gurin, Journal of the American Chemical Society, 1935, vol. 57, p. 1879