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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