3 years ago

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

3-Hydroxy-N′-arylidenepropanehydrazonamides with Halo-Substituted Phenanthrene Scaffolds Cure P. berghei Infected Mice When Administered Perorally
Krystina Kuna, Christoph Fischli, Sergio Wittlin, Diane Meitzner, Benjamin Mordmüller, Tanja C. Knaab, Sandra Duffy, Jana Held, Vicky M. Avery, Mirko Buchholz, Beate Lungerich, Stephan Meister, Elizabeth A. Winzeler, Michael Leven, Petra Stahlke, Ursula Lehmann, Michael J. Delves, Thomas Kurz
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.

Publisher URL: http://dx.doi.org/10.1021/acs.jmedchem.7b00140

DOI: 10.1021/acs.jmedchem.7b00140

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