Mono- and bis-thiazolium salts have potent antimalarial activity
Mono- and bis-thiazolium salts have potent antimalarial activity
复制标题
DOI：
10.1021/jm0492608
复制
发表时间：
2005-05-19
影响因子：
7.3
通讯作者：
Calas, M
中科院分区：
文献类型：
--
作者：
Hamzé, A;Rubi, E;Calas, M
合成了由单或双（N或c -5）噻唑盐组成的24种新型阳离子胆碱类似物的三个新系列。双噻唑盐显示出有效的抗疟活性（远优于单噻唑盐）。其中双噻唑盐12和13对恶性疟原虫的IC50值分别为2.25 nM和0.65 nM。这些化合物还显示出良好的体内活性（ED50）
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