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Current Pharmaceutical Design

Volume 18 Issue 24
ISSN: 1381-6128
eISSN: 1873-4286


   All Titles

  Choline Analogues in Malaria Chemotherapy
  pp.3454-3466 (13) Authors: Suzanne Peyrottes, Sergio Caldarelli, Sharon Wein, Christian Perigaud, Alain Pellet, Henri Vial

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.
  Key: New Content Free Content Open Access Plus Subscribed Content

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