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.
Keywords: Malaria, plasmodium, phospholipid, choline analogues, quaternary ammonium, thiazolium salts, pharmacology, anti-malaria drugs, Albitiazolium, prodrug
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