%0 Journal Article
%9 ACL : Articles dans des revues avec comité de lecture répertoriées par l'AERES
%A Rivaud, M.
%A Mendoza, A.
%A Sauvain, Michel
%A Valentin, A.
%A Jullian, Valérie
%T Short synthesis and antimalarial activity of fagaronine
%D 2012
%L fdi:010057058
%G ENG
%J Bioorganic and Medicinal Chemistry
%@ 0968-0896
%K Fagaronine ; Benzo[c]phenanthridine ; Synthesis ; Malaria ; In vivo experiment
%M ISI:000306480200029
%N 15
%P 4856-4861
%R 10.1016/j.bmc.2012.05.061
%U https://www.documentation.ird.fr/hor/fdi:010057058
%> https://www.documentation.ird.fr/intranet/publi/2012/08/010057058.pdf
%V 20
%W Horizon (IRD)
%X 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.
%$ 052 ; 050 ; 020