title: Choline analogues in malaria chemotherapy.
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.
authors.affiliation: Institut des Biomolécules Max Mousseron, UMR 5247 CNRS-UM1-UM2, Université Montpellier 2, place E. Bataillon, 34095 Montpellier, France. peyrottes@univ-montp2.fr
authors.forename: Suzanne
authors.initials: S
authors.lastname: Peyrottes
authors.forename: Sergio
authors.initials: S
authors.lastname: Caldarelli
authors.forename: Sharon
authors.initials: S
authors.lastname: Wein
authors.forename: Christian
authors.initials: C
authors.lastname: Périgaud
authors.forename: Alain
authors.initials: A
authors.lastname: Pellet
authors.forename: Henri
authors.initials: H
authors.lastname: Vial
mesh_terms: D000818:Animals; D000962:Antimalarials / Q000627:therapeutic use*; D002794:Choline / Q000031:analogs & derivatives* / Q000627:therapeutic use*; D006801:Humans; D008288:Malaria / Q000188:drug therapy* / Q000469:parasitology; D010965:Plasmodium malariae / Q000187:drug effects*
chemical_list: D000962:Antimalarials; D002794:Choline