Sialidase inhibitors related to zanamivir. Further SAR studies of 4-amino-4H-pyran-2-carboxylic acid-6-propylamides

Paul G. Wyatt, Barry A. Coomber, Derek N. Evans, Torquil I. Jack, Heather E. Fulton, Alan J. Wonacott, Peter Colman, Jose Varghese

    Research output: Contribution to journalArticle

    47 Citations (Scopus)

    Abstract

    SAR investigations of the 4- and 5-positions of a series of 4-amino-4H-pyran-2-carboxylic acid 6-carboxamides are reported. Potent inhibitors of influenza A sialidase with marked selectivity over the influenza B enzyme were obtained when the basic 4-amino substituent was replaced by hydroxyl or even deleted. Modifications at the 5-position exhibited a tight steric requirement, with trifluoroacetamide being optimal.
    Original languageEnglish
    Pages (from-to)669-673
    Number of pages5
    JournalBioorganic & Medicinal Chemistry Letters
    Volume11
    Issue number5
    DOIs
    Publication statusPublished - Mar 2001

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