Mono- and Bis-Thiazolium Salts Have Potent Antimalarial Activity
2005; American Chemical Society; Volume: 48; Issue: 10 Linguagem: Inglês
10.1021/jm0492608
ISSN1520-4804
AutoresAbdallah Hamzé, Eric Rubi, Pascal Arnal, Michel Boisbrun, Carole Carcel, Xavier J. Salom‐Roig, Marjorie Maynadier, Sharon Wein, Henri Vial, Michèle Calas,
Tópico(s)Synthesis and Catalytic Reactions
ResumoThree 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.
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