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3-Hydroxy-N '-arylidenepropanehydrazonamides with Halo-Substituted Phenanthrene Scaffolds Cure P. berghei Infected Mice When Administered Perorally

: Leven, M.; Knaab, T.C.; Held, J.; Duffy, S.; Meister, S.; Fischli, C.; Meitzner, D.; Lehmann, U.; Lungerich, B.; Kuna, K.; Stahlke, P.; Delves, M.; Buchholz, M.; Winzeler, E.A.; Avery, V.M.; Mordmüller, B.; Wittlin, S.; Kurz, T.


Journal of medicinal chemistry 60 (2017), No.14, pp.6036-6044
ISSN: 0022-2623
ISSN: 1520-4804
Journal Article
Fraunhofer IZI ()

Structural optimization of 3-hydroxy-N'-arylidenepropanehydrazonamides provided new analogs with nanomolar to subnanomolar antiplasmodial activity against asexual blood stages of Plasmodium falciparum, excellent parasite selectivity, and nanomolar activity against the earliest forms of gametocyte development. Particularly, derivatives with a 1,3-dihalo-6-trifluoromethylphenanthrene moiety showed outstanding in vivo properties and demonstrated in part curative activity in the Plasmodium berghei mouse model when administered perorally.