Glutathione-like tripeptides as inhibitors of glutathionylspermidine synthetase. Part 1: Substitution of the glycine carboxylic acid group

Katie Amssoms, Sandra Oza, Esteban Ravaschino, Abdellah Yamani, Anne Marie Lambeir, Padinchare Rajan, Gunther Bal, Juan Bautista Rodriguez, Alan H. Fairlamb, Achiel Haemers (Lead / Corresponding author)

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    24 Citations (Scopus)

    Abstract

    Glutathionylspermidine synthetase/amidase (GspS) is an essential enzyme in the biosynthesis and turnover of trypanothione and represents an attractive target for the design of selective anti-parasitic drugs. We synthesised a series of analogues of glutathione (L-γ-Glu-L-Leu-Gly-X) where the glycine carboxylic acid group (X) has been substituted for other acidic groups such as tetrazole, hydroxamic acid, acylsulphonamide and boronic acid. The boronic acid appears the most promising lead compound (IC50 of 17.2 µM).
    Original languageEnglish
    Pages (from-to)2553-2556
    Number of pages4
    JournalBioorganic & Medicinal Chemistry Letters
    Volume12
    Issue number18
    DOIs
    Publication statusPublished - 16 Sep 2002

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