Inhibition of trypanothione reductase and glutathione reductase by ferrocenic 4-aminoquinoline ureas

Margaret A. L. Blackie, Ahilan Saravanamuthu, Alan H. Fairlamb, Kelly Chibale

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    5 Citations (Scopus)

    Abstract

    New ferrocenic 4-aminoquinoline urea compounds have been tested for inhibition of trypanothione reductase (TryR) and human glutathione reductase (GR). Several compounds were also tested in vitro against Leishmania donovani, Trypanosoma cruzi and Trypanosoma brucei rhodesiense. All compounds showed significant improvement in inhibition of TryR relative to chloroquine with the best compound showing an IC50 value of 2.4 mu M (Chloroquine IC50 = 47.6 mu M).

    Original languageEnglish
    Pages (from-to)52-60
    Number of pages9
    JournalARKIVOC
    Volume2008
    Issue numbervi
    Publication statusPublished - 2008

    Keywords

    • Ferroquine
    • 7-chloroquinoline
    • urea
    • in vitro
    • trypanothione reductase
    • ACTIVITY IN-VITRO
    • TRYPANOSOMA-CRUZI
    • CRITHIDIA-FASCICULATA
    • ANALOGS
    • ANTIPROTOZOAL
    • LEISHMANIA
    • QUINACRINE
    • DISCOVERY
    • MALARIA
    • DESIGN

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