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  • 2,4-Diaminothienopyrimidines as orally active antimalarial agents

    Author(s)
    Cabrera, Diego Gonzalez
    Le Manach, Claire
    Douelle, Frederic
    Younis, Yassir
    Feng, Tzu-Shean
    Paquet, Tanya
    Nchinda, Aloysius T
    Street, Leslie J
    Taylor, Dale
    de Kock, Carmen
    Wiesner, Lubbe
    Duffy, Sandra
    White, Karen L
    Zabiulla, K Mohammed
    Sambandan, Yuvaraj
    Bashyam, Sridevi
    Waterson, David
    Witty, Michael J
    Charman, Susan A
    Avery, Vicky M
    Wittlin, Sergio
    Chibale, Kelly
    Griffith University Author(s)
    Duffy, Sandra
    Avery, Vicky M.
    Year published
    2014
    Metadata
    Show full item record
    Abstract
    A novel series of 2,4-diaminothienopyrimidines with potential as antimalarials was identified from whole-cell high-throughput screening of a SoftFocus ion channel library. Synthesis and structure–activity relationship studies identified compounds with potent antiplasmodial activity and low in vitro cytotoxicity. Several of these analogues exhibited in vivo activity in the Plasmodium berghei mouse model when administered orally. However, inhibition of the hERG potassium channel was identified as a liability for this series.A novel series of 2,4-diaminothienopyrimidines with potential as antimalarials was identified from whole-cell high-throughput screening of a SoftFocus ion channel library. Synthesis and structure–activity relationship studies identified compounds with potent antiplasmodial activity and low in vitro cytotoxicity. Several of these analogues exhibited in vivo activity in the Plasmodium berghei mouse model when administered orally. However, inhibition of the hERG potassium channel was identified as a liability for this series.
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    Journal Title
    Journal of Medicinal Chemistry
    Volume
    57
    Issue
    3
    DOI
    https://doi.org/10.1021/jm401760c
    Subject
    Medicinal and biomolecular chemistry
    Medicinal and biomolecular chemistry not elsewhere classified
    Organic chemistry
    Pharmacology and pharmaceutical sciences
    Publication URI
    http://hdl.handle.net/10072/102413
    Collection
    • Journal articles

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