十一异戊烯基焦磷酸合酶（UPPS）强效和选择性抑制剂的设计及构效关系：四嗪酸、特窗酸和二氢吡啶 - 2 - 酮
Design and structure-activity relationships of potent and selective inhibitors of undecaprenyl pyrophosphate synthase (UPPS): tetramic, tetronic acids and dihydropyridin-2-ones.
作者信息
Peukert Stefan, Sun Yingchuan, Zhang Rui, Hurley Brian, Sabio Mike, Shen Xiaoyu, Gray Christen, Dzink-Fox JoAnn, Tao Jianshi, Cebula Regina, Wattanasin Sompong
机构信息
Novartis Institutes for BioMedical Research, Inc., 250 Massachusetts Avenue, Cambridge, MA 02139, USA.
出版信息
Bioorg Med Chem Lett. 2008 Mar 15;18(6):1840-4. doi: 10.1016/j.bmcl.2008.02.009. Epub 2008 Feb 10.
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.
基于药效团假说，研究了取代的四胺酸和四酮酸3-羧酰胺以及二氢吡啶-2-酮-3-羧酰胺作为十一异戊烯基焦磷酸合酶（UPPS）抑制剂，用作新型抗菌剂。讨论了这类化合物的合成及构效关系模式。提供了所选化合物的选择性数据和抗菌活性。
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