A new potent inhibitor of fungal melanin biosynthesis identified through combinatorial chemistry

Lee D. Jennings*, Zdzislaw Wawrzak, Denise Amorose, Rand S. Schwartz, Douglas B. Jordan

*Corresponding author for this work

    Research output: Contribution to journalArticlepeer-review

    20 Scopus citations

    Abstract

    A new fungicide lead has been identified by in vitro screening of a focused combinatorial library. Amides (768) were synthesized in pools of four and assayed as inhibitors of scytalone dehydratase. Deconvolution of one of the most active pools led to the discovery of a potent inhibitor of the enzyme 3b (K(i) = 26 pM), which has fungicidal properties.

    Original languageEnglish (US)
    Pages (from-to)2509-2514
    Number of pages6
    JournalBioorganic and Medicinal Chemistry Letters
    Volume9
    Issue number17
    DOIs
    StatePublished - Sep 6 1999

    ASJC Scopus subject areas

    • Biochemistry
    • Molecular Medicine
    • Molecular Biology
    • Pharmaceutical Science
    • Drug Discovery
    • Clinical Biochemistry
    • Organic Chemistry

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