Mono- and Bis-Thiazolium Salts Have Potent Antimalarial Activity
- 15 April 2005
- journal article
- research article
- Published by American Chemical Society (ACS) in Journal of Medicinal Chemistry
- Vol. 48 (10) , 3639-3643
- https://doi.org/10.1021/jm0492608
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 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.Keywords
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