Choline Analogues in Malaria Chemotherapy

Author(s): Suzanne Peyrottes, Sergio Caldarelli, Sharon Wein, Christian Perigaud, Alain Pellet, Henri Vial.

Journal Name: Current Pharmaceutical Design

Volume 18 , Issue 24 , 2012

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

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Article Details

VOLUME: 18
ISSUE: 24
Year: 2012
Page: [3454 - 3466]
Pages: 13
DOI: 10.2174/138161212801327338

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