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Choline Analogues in Malaria Chemotherapy

[ Vol. 18 , Issue. 24 ]

Author(s):

Suzanne Peyrottes, Sergio Caldarelli, Sharon Wein, Christian Perigaud, Alain Pellet and Henri Vial   Pages 3454 - 3466 ( 13 )

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

Affiliation:

Institut des Biomolecules Max Mousseron (IBMM), UMR 5247 CNRS-UM1-UM2, Universite Montpellier 2, place E. Bataillon, 34095 Montpellier, France.



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