Short synthesis and antimalarial activity of fagaronine |
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| Authors: | M Rivaud A Mendoza M Sauvain A Valentin V Jullian |
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| Institution: | 1. Université de Toulouse, UPS, UMR 152 (Laboratoire Pharmadev), Faculté de Pharmacie, 35, chemin des maraîchers, F-31062 Toulouse cedex 9, France;2. Institut de Recherche pour le Développement (IRD), UMR 152 (Laboratoire Pharmadev), 118, rte de Narbonne, F-31062 Toulouse cedex 9, France;3. Unidad en Investigación y Desarrollo de Medicamentos, Centro de Investigación en Farmacobiologia Aplicada (CIFA), Universidad de Navarra, c/Irunlarrea s/n, 31080 Pamplona, Spain;4. Institut de Recherche pour le Développement (IRD), UMR 152, Mission IRD Casilla 18-1209, Lima, Peru |
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| 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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