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

被引：22

作者：

Jennings, LD

Wawrzak, Z

Amorose, D

Schwartz, RS

Jordan, DB

机构：

[1] DuPont Agr Prod, Stine Haskell Res Ctr, Newark, DE 19714 USA

[2] DuPont Cent Res & Dev, Expt Stn, Wilmington, DE 19880 USA

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 1999年 / 9卷 / 17期

关键词：

D O I：

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

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

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 Science Ltd. All rights reserved.

引用

页码：2509 / 2514

页数：6

共 20 条

[1] Crystal structure of the ternary complex of 1,3,8-trihydroxynaphthalene reductase from Magnaporthe grisea with NADPH and an active-site inhibitor [J].