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  • Identification and In-Vitro ADME Assessment of a Series of Novel Anti-Malarial Agents Suitable for Hit-to-Lead Chemistry

    Author(s)
    Edlin, Chris D
    Morgans, Garreth
    Winks, Susan
    Duffy, Sandra
    Avery, Vicky M
    Wittlin, Sergio
    Waterson, David
    Burrows, Jeremy
    Bryans, Justin
    Griffith University Author(s)
    Duffy, Sandra
    Avery, Vicky M.
    Year published
    2012
    Metadata
    Show full item record
    Abstract
    Triage of a set of antimalaria hit compounds, identified through high throughput screening against the Chloroquine sensitive (3D7) and resistant (Dd2) parasite Plasmodium falciparum strains identified several novel chemotypes suitable for hit-to-lead chemistry investigation. The set was further refined through investigation of their in vitro ADME properties, which identified templates with good potential to be developed further as antimalarial agents. One example was profiled in an in vivo murine Plasmodium berghei model of malaria infection.Triage of a set of antimalaria hit compounds, identified through high throughput screening against the Chloroquine sensitive (3D7) and resistant (Dd2) parasite Plasmodium falciparum strains identified several novel chemotypes suitable for hit-to-lead chemistry investigation. The set was further refined through investigation of their in vitro ADME properties, which identified templates with good potential to be developed further as antimalarial agents. One example was profiled in an in vivo murine Plasmodium berghei model of malaria infection.
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    Journal Title
    ACS Medicinal Chemistry Letters
    Volume
    3
    DOI
    https://doi.org/10.1021/ml300091c
    Copyright Statement
    Self-archiving of the author-manuscript version is not yet supported by this journal. Please refer to the journal link for access to the definitive, published version or contact the authors for more information.
    Subject
    Medicinal and Biomolecular Chemistry not elsewhere classified
    Organic Chemistry not elsewhere classified
    Medicinal and Biomolecular Chemistry
    Organic Chemistry
    Pharmacology and Pharmaceutical Sciences
    Publication URI
    http://hdl.handle.net/10072/52013
    Collection
    • Journal articles

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