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

    Author
    Leven, Michael
    Knaab, Tanja C.
    Held, Jana
    Duffy, Sandra
    Meister, Stephan
    Fischli, Christoph
    Meitzner, Diane
    Lehmann, Ursula
    Lungerich, Beate
    Kuna, Krystina
    Stahlke, Petra
    Delves, Michael J.
    Buchholz, Mirko
    Winzeler, Elizabeth A.
    Avery, Vicky
    Mordmüller, Benjamin
    Wittlin, Sergio
    Kurz, Thomas
    Year published
    2017
    Metadata
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    Abstract
    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.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.
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    Journal Title
    Journal of Medicinal Chemistry
    Volume
    60
    Issue
    14
    DOI
    https://doi.org/10.1021/acs.jmedchem.7b00140
    Subject
    Medicinal and Biomolecular Chemistry not elsewhere classified
    Publication URI
    http://hdl.handle.net/10072/351638
    Collection
    • Journal articles

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