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  • 8-Aminoquinolines with an Aminoxyalkyl Side Chain Exert in vitro Dual-Stage Antiplasmodial Activity

    Author(s)
    Leven, Michael
    Held, Jana
    Duffy, Sandra
    Avelar, Leandro A Alves
    Meister, Stephan
    Delves, Michael
    Plouffe, David
    Kuna, Krystina
    Tschan, Serena
    Avery, Vicky M
    Winzeler, Elizabeth A
    Mordmueller, Benjamin
    Kurz, Thomas
    Griffith University Author(s)
    Duffy, Sandra
    Avery, Vicky M.
    Year published
    2019
    Metadata
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    Abstract
    A series of novel 8‐aminoquinolines (8‐AQs) with an aminoxyalkyl side chain were synthesized and evaluated for in vitro antiplasmodial properties against asexual blood stages, liver stages, and sexual stages of Plasmodium falciparum. 8‐AQs bearing 2‐alkoxy and 5‐phenoxy substituents on the quinoline ring system were found to be the most promising compounds under study, exhibiting potent blood schizontocidal and moderate tissue schizontocidal in vitro activity.A series of novel 8‐aminoquinolines (8‐AQs) with an aminoxyalkyl side chain were synthesized and evaluated for in vitro antiplasmodial properties against asexual blood stages, liver stages, and sexual stages of Plasmodium falciparum. 8‐AQs bearing 2‐alkoxy and 5‐phenoxy substituents on the quinoline ring system were found to be the most promising compounds under study, exhibiting potent blood schizontocidal and moderate tissue schizontocidal in vitro activity.
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    Journal Title
    CHEMMEDCHEM
    Volume
    14
    Issue
    4
    DOI
    https://doi.org/10.1002/cmdc.201800691
    Subject
    Medicinal and biomolecular chemistry
    Organic chemistry
    Pharmacology and pharmaceutical sciences
    Publication URI
    http://hdl.handle.net/10072/383319
    Collection
    • Journal articles

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