2. Academic Validation
  3. Short synthesis and antimalarial activity of fagaronine

Short synthesis and antimalarial activity of fagaronine

  • Bioorg Med Chem. 2012 Aug 1;20(15):4856-61. doi: 10.1016/j.bmc.2012.05.061.
M Rivaud 1,  A Mendoza,  M Sauvain,  A Valentin,  V Jullian
Affiliations

Affiliation

  • 1 Université de Toulouse, UPS, UMR 152 (Laboratoire Pharmadev), Faculté de Pharmacie, 35, chemin des maraîchers, F-31062 Toulouse cedex 9, France.
PMID: 22766218 DOI: 10.1016/j.bmc.2012.05.061
Abstract

Herein, we report a new synthesis of fagaronine 1, inspired by the synthesis reported by Luo for nornitidine. The in vitro biological activity of fagaronine against malaria on several chloroquine-sensitive and resistant Plasmodium falciparum strains was confirmed, and the selectivity index compared to mammalian cells was calculated. Fagaronine was found to have very good antimalarial activity in vivo, comparable to the activity of the reference compound chloroquine. Therefore, fagaronine appears to be a good potential lead for the design of new antimalarial molecules.

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