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

Authors
Jennings, LD Wawrzak, Z Amorose, D Schwartz, RS Jordan, DB
Citation
Ld. Jennings et al., A new potent inhibitor of fungal melanin biosynthesis identified through combinatorial chemistry, BIOORG MED, 9(17), 1999, pp. 2509-2514
Citations number
16
Categorie Soggetti
Chemistry & Analysis
Journal title
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
ISSN journal
0960894X → ACNP
Volume
9
Issue
17
Year of publication
1999
Pages
2509 - 2514
Database
ISI
SICI code
0960-894X(19990906)9:17<2509:ANPIOF>2.0.ZU;2-3
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. (C) 1999 Elsevier Scien ce Ltd. All rights reserved.