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    Scoping Studies into the Structure-Activity Relationship (SAR) of Phenylephrine-Derived Analogues as Inhibitors of Trypanosoma brucei rhodesiense

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    Fulltext not available
    Authors
    Cullen, Danica
    Pengon, J.
    Rattanajak, R.
    Chaplin, J.
    Kamchonwongpaisan, S.
    Mocerino, Mauro
    Date
    2016
    Type
    Journal Article
    
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    Citation
    Cullen, D. and Pengon, J. and Rattanajak, R. and Chaplin, J. and Kamchonwongpaisan, S. and Mocerino, M. 2016. Scoping Studies into the Structure-Activity Relationship (SAR) of Phenylephrine-Derived Analogues as Inhibitors of Trypanosoma brucei rhodesiense. ChemistrySelect. 1 (15): pp. 4533-4538.
    Source Title
    ChemistrySelect
    ISSN
    2365-6549
    School
    Department of Chemistry
    URI
    http://hdl.handle.net/20.500.11937/51609
    Collection
    • Curtin Research Publications
    Abstract

    Human African Trypanosomiasis (HAT) is a disease caused by the parasite Trypanosoma brucei and is classified as a neglected tropical disease of concern in sub-Saharan Africa. A scoping study has been undertaken to develop a preliminary structure activity relationship of a tetrahydroisoquinoline scaffold. Fourteen compounds based around this core scaffold were synthesised and evaluated for their activity against Trypanosoma brucei rhodesiense in vitro. Initial results are promising with a number of analogues showing low micromolar inhibition of T.b.rhodesiense with acceptable selectivity over mammalian cells. The most promising is a secondary amine analogue showing the most potent inhibition of T.b.rhodesiense, with an IC50 value of 0.25 ± 0.02 µM, while also showing low cytotoxicity to mammalian cells.

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