Benzoic acid and pyridine derivatives as inhibitors of Trypanosoma cruzi trans-sialidase

João Neres, Pascal Bonnet, Philip N. Edwards, Pravin L. Kotian, Alejandro Buschiazzo, Pedro M. Alzari, Richard A. Bryce, Kenneth T. Douglas

    Research output: Contribution to journalArticlepeer-review

    Abstract

    Benzoic acid and pyridine derivatives inhibit recombinant trans-sialidase from Trypanosoma cruzi with I50 values between 0.4 and 1 mM. The best compounds, 4-acetylamino-3-hydroxymethylbenzoic acid and 5-acetylamino-6-aminopyridine-2-carboxylic acid, provide new leads to inhibitors not containing the synthetically complex sialic acid structure. The weak inhibition by such compounds contrasts with their much stronger inhibition of neuraminidase from Influenza virus. © 2007 Elsevier Ltd. All rights reserved.
    Original languageEnglish
    Pages (from-to)2106-2119
    Number of pages13
    JournalBioorganic and Medicinal Chemistry
    Volume15
    Issue number5
    DOIs
    Publication statusPublished - 1 Mar 2007

    Keywords

    • Chagas disease
    • Inhibitors
    • Neuraminidase
    • Trans-sialidase

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