Design and structure-activity relationships of potent and selective inhibitors of undecaprenyl pyrophosphate synthase (UPPS): Tetramic, tetronic acids and dihydropyridin-2-ones
Design and structure-activity relationships of potent and selective inhibitors of undecaprenyl pyrophosphate synthase (UPPS): Tetramic, tetronic acids and dihydropyridin-2-ones
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DOI：
10.1016/j.bmcl.2008.02.009
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发表时间：
2008-03-15
影响因子：
2.7
通讯作者：
Wattanasin, Sompong
中科院分区：
文献类型：
--
作者：
Peukert, Stefan;Sun, Yingchuan;Wattanasin, Sompong
基于药效团假说，研究了取代的特特拉姆和特窗酸3-羧酰胺以及二氢吡啶-2-酮-3-羧酰胺作为十一异戊二烯焦磷酸合酶（UPPS）抑制剂用作新型抗菌剂。并对该类化合物的合成及构效关系进行了讨论.提供了所选化合物的选择性数据和抗菌活性。(C)2008爱思唯尔有限公司保留所有权利。
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.