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Free Content Choline Analogues in Malaria Chemotherapy

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

Document Type: Research Article

Publication date: August 1, 2012

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