High-throughput screening affords novel and selective trypanothione reductase inhibitors with anti-trypanosomal activity

Derek C. Martyn, Deuan C. Jones, Alan H. Fairlamb, Jon Clardy (Lead / Corresponding author)

    Research output: Contribution to journalArticlepeer-review

    41 Citations (Scopus)

    Abstract

    Trypanothione reductase (TR), an enzyme that buffers oxidative stress in trypanosomatid parasites, was screened against commercial libraries containing approximately 134,500 compounds. After secondary screening, four chemotypes were identified as screening positives with selectivity for TR over human glutathione reductase. Thirteen compounds from these four chemotypes were purchased, and their in vitro activity against TR and Trypanosoma brucei is described.

    Original languageEnglish
    Pages (from-to)1280-1283
    Number of pages4
    JournalBioorganic and Medicinal Chemistry Letters
    Volume17
    Issue number5
    DOIs
    Publication statusPublished - 1 Mar 2007

    Keywords

    • High-throughput screening
    • Trypanosomiasis
    • Trypanothione reductase

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