1.
J Med Chem
; 48(10): 3639-43, 2005 May 19.
Artículo
en Inglés
| MEDLINE
| ID: mdl-15887971
RESUMEN
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) = 0.22 mg/kg), and low toxicity in mice infected by Plasmodium vinckei.