Mono- and bis-thiazolium salts have potent antimalarial activity.
J Med Chem
; 48(10): 3639-43, 2005 May 19.
Article
en En
| MEDLINE
| ID: mdl-15887971
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 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.
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Colección:
01-internacional
Banco de datos:
MEDLINE
Asunto principal:
Tiazoles
/
Antimaláricos
Límite:
Animals
Idioma:
En
Revista:
J Med Chem
Asunto de la revista:
QUIMICA
Año:
2005
Tipo del documento:
Article
País de afiliación:
Francia