Design and structure-activity relationships of potent and selective inhibitors of undecaprenyl pyrophosphate synthase (UPPS): Tetramic, tetronic acids and dihydropyridin-2-ones

被引：86

作者：

Peukert, Stefan ^{[1
]}

Sun, Yingchuan ^{[1
]}

Zhang, Rui ^{[1
]}

Hurley, Brian ^{[1
]}

Sabio, Mike ^{[1
]}

Shen, Xiaoyu ^{[1
]}

Gray, Christen ^{[1
]}

Dzink-Fox, Joann ^{[1
]}

Tao, Jianshi ^{[1
]}

Cebula, Regina ^{[1
]}

Wattanasin, Sompong ^{[1
]}

机构：

[1] BioMed Res Inc, Novartis Inst, Cambridge, MA 02139 USA

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2008年 / 18卷 / 06期

关键词：

Antibacterial; Undecaprenyl pyrophosphate synthase; UPPS inhibitor;

D O I：

10.1016/j.bmcl.2008.02.009

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

Based on a pharmacophore hypothesis substituted tetramic and tetronic acid 3-carboxamides as well as dihydropyridin-2-one- 3-carboxamides were investigated as inhibitors of undecaprenyl pyrophosphate synthase (UPPS) for use as novel antimicrobial agents. Synthesis and structure - activity relationship patterns for this class of compounds are discussed. Selectivity data and antibacterial activities for selected compounds are provided. (C) 2008 Elsevier Ltd. All rights reserved.

引用

页码：1840 / 1844

页数：5

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