Antiprotozoal and cytotoxicity evaluation of sulfonamide and urea analogues of quinacrine

Kelly Chibale (Lead / Corresponding author), Hayley Haupt, Howard Kendrick, Vanessa Yardley, Ahilan Saravanamuthu, Alan H. Fairlamb, Simon L. Croft

    Research output: Contribution to journalArticlepeer-review

    94 Citations (Scopus)

    Abstract

    Sulfonamide and urea derivatives of quinacrine with varying methylene spacer lengths were synthesised and tested for inhibition of trypanothione reductase (TryR) and for activity in vitro against strains of the parasitic protozoa Trypanosoma, Leishmania, and Plasmodium. These derivatives are superior inhibitors of TryR relative to quinacrine with the best compound being 40 times more potent. Urea derivatives generally displayed good in vitro activity against all parasites.

    Original languageEnglish
    Pages (from-to)2655-2657
    Number of pages3
    JournalBioorganic and Medicinal Chemistry Letters
    Volume11
    Issue number19
    DOIs
    Publication statusPublished - 8 Oct 2001

    ASJC Scopus subject areas

    • Biochemistry
    • Molecular Medicine
    • Molecular Biology
    • Pharmaceutical Science
    • Drug Discovery
    • Clinical Biochemistry
    • Organic Chemistry

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