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Rivaud M., Mendoza A., Sauvain Michel, Valentin A., Jullian Valérie. (2012). Short synthesis and antimalarial activity of fagaronine. Bioorganic and Medicinal Chemistry, 20 (15), p. 4856-4861. ISSN 0968-0896.

Titre du document
Short synthesis and antimalarial activity of fagaronine
Année de publication
2012
Type de document
Article référencé dans le Web of Science WOS:000306480200029
Auteurs
Rivaud M., Mendoza A., Sauvain Michel, Valentin A., Jullian Valérie
Source
Bioorganic and Medicinal Chemistry, 2012, 20 (15), p. 4856-4861 ISSN 0968-0896
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.
Plan de classement
Sciences fondamentales / Techniques d'analyse et de recherche [020] ; Santé : généralités [050] ; Entomologie médicale / Parasitologie / Virologie [052]
Localisation
Fonds IRD [F B010057058]
Identifiant IRD
fdi:010057058
Contact