Abstract
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
Current Pharmaceutical Design
Title:Choline Analogues in Malaria Chemotherapy
Volume: 18 Issue: 24
Author(s): Suzanne Peyrottes, Sergio Caldarelli, Sharon Wein, Christian Perigaud, Alain Pellet and Henri Vial
Affiliation:
Keywords: Malaria, plasmodium, phospholipid, choline analogues, quaternary ammonium, thiazolium salts, pharmacology, anti-malaria drugs, Albitiazolium, prodrug
Abstract: 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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Cite this article as:
Peyrottes Suzanne, Caldarelli Sergio, Wein Sharon, Perigaud Christian, Pellet Alain and Vial Henri, Choline Analogues in Malaria Chemotherapy, Current Pharmaceutical Design 2012; 18 (24) . https://dx.doi.org/10.2174/138161212801327338
DOI https://dx.doi.org/10.2174/138161212801327338 |
Print ISSN 1381-6128 |
Publisher Name Bentham Science Publisher |
Online ISSN 1873-4286 |
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