Suzanne Peyrottes, Sergio Caldarelli, Sharon Wein, Christian Perigaud, Alain Pellet and Henri Vial Pages 3454 - 3466 ( 13 )
Emerging resistance against well-established anti-malaria drugs warrants the introduction of new therapeutic agents with original mechanisms of action. Inhibition of membrane-based phospholipid biosynthesis, which is crucial for the parasite, has thus been proposed as a novel and promising therapeutic strategy. This review compiles literature concerning the design and study of choline analogues and related cation derivatives as potential anti-malarials. It covers advances achieved over the last two decades and describes: the concept validation, the design and selection of a clinical candidate (Albitiazolium), back-up derivatives while also providing insight into the development of prodrug approaches.
Malaria, plasmodium, phospholipid, choline analogues, quaternary ammonium, thiazolium salts, pharmacology, anti-malaria drugs, Albitiazolium, prodrug
Institut des Biomolecules Max Mousseron (IBMM), UMR 5247 CNRS-UM1-UM2, Universite Montpellier 2, place E. Bataillon, 34095 Montpellier, France.