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

doi:10.1016/S0960-894X(99)00424-2

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 journal › Article › peer-review

25 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 language	English (US)
Pages (from-to)	2509-2514
Number of pages	6
Journal	Bioorganic and Medicinal Chemistry Letters
Volume	9
Issue number	17
DOIs	https://doi.org/10.1016/S0960-894X(99)00424-2
State	Published - Sep 6 1999
Externally published	Yes

ASJC Scopus subject areas

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

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10.1016/S0960-894X(99)00424-2

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

Abstract

ASJC Scopus subject areas

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