title: Short synthesis and antimalarial activity of fagaronine.
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.
authors: Université de Toulouse, UPS, UMR 152 (Laboratoire Pharmadev), Faculté de Pharmacie, 35, chemin des maraîchers, F-31062 Toulouse cedex 9, France.
authors: M
authors: M
authors: Rivaud
authors: A
authors: A
authors: Mendoza
authors: M
authors: M
authors: Sauvain
authors: A
authors: A
authors: Valentin
authors: V
authors: V
authors: Jullian
mesh_terms: D000818:Animals; D000962:Antimalarials / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D053119:Benzophenanthridines / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D002522:Chlorocebus aethiops; D002738:Chloroquine / Q000494:pharmacology; D004195:Disease Models, Animal; D004305:Dose-Response Relationship, Drug; D004351:Drug Resistance / Q000187:drug effects*; D005260:Female; D051379:Mice; D015394:Molecular Structure; D021261:Parasitic Sensitivity Tests; D010963:Plasmodium falciparum / Q000187:drug effects*; D013329:Structure-Activity Relationship; D014709:Vero Cells
chemical_list: D000962:Antimalarials; D053119:Benzophenanthridines; C002066:fagaronine; D002738:Chloroquine