22339-61-3Relevant articles and documents
Mono- and bis-thiazolium salts have potent antimalarial activity
Hamzé, Abdallah,Rubi, Eric,Arnal, Pascal,Boisbrun, Michel,Carcel, Carole,Salom-Roig, Xavier,Maynadier, Marjorie,Wein, Sharon,Vial, Henri,Calas, Michèle
, p. 3639 - 3643 (2005)
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.