Exploring the potential of xanthene derivatives as trypanothione reductase inhibitors and chloroquine potentiating agents

Kelly Chibale (Lead / Corresponding author), Mark Visser, Donelly van Schalkwyk, Peter J. Smith, Ahilan Saravanamuthu, Alan H. Fairlamb

    Research output: Contribution to journalArticlepeer-review

    182 Citations (Scopus)

    Abstract

    Xanthene derivatives were synthesized and evaluated for their potential as trypanothione reductase (TryR) inhibitors and chloroquine (CQ) potentiating agents. Some derivatives displayed inhibitory activity against TryR comparable to known tricyclic anti-depressants. On the other hand a number of derivatives increased CQ accumulation and potentiating effects in a resistant strain of Plasmodium falciparum with one compound also displaying strong intrinsic antimalarial activity.

    Original languageEnglish
    Pages (from-to)2289-2296
    Number of pages8
    JournalTetrahedron
    Volume59
    Issue number13
    DOIs
    Publication statusPublished - 24 Mar 2003

    Keywords

    • 9,9-dimethylxanthenes
    • Chloroquine potentiating agents
    • Leishmaniasis
    • Malaria
    • Trypanosomiasis
    • Trypanothione reductase inhibitors

    ASJC Scopus subject areas

    • Biochemistry
    • Drug Discovery
    • Organic Chemistry

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