1,3-Dioxane-Linked Novel Bacterial Topoisomerase Inhibitors: Expanding Structural Diversity and the Antibacterial Spectrum.
1,3-Dioxane-Linked Novel Bacterial Topoisomerase Inhibitors: Expanding Structural Diversity and the Antibacterial Spectrum.
复制标题
1,3-二恶烷连接的新型细菌拓扑异构酶抑制剂：扩大结构多样性和抗菌谱。
DOI：
10.1021/acsmedchemlett.2c00111
复制
发表时间：
2022
影响因子：
4.2
通讯作者：
Wozniak,D
中科院分区：
文献类型：
--
作者：
Lu,Yanran;Mann,ChelseaA;Nolan,Sheri;Collins,JessicaA;Parker,Elizabeth;Papa,Jonathan;Vibhute,Sandip;Jahanbakhsh,Seyedehameneh;Thwaites,Mary;Hufnagel,David;Hazbón,ManzourH;Moreno,Jane;Stedman,TimothyT;Wittum,Thomas;Wozniak,D
抗生素耐药性继续破坏现有的治疗方法。新型细菌拓扑异构酶抑制剂（NBTI）为这一关键问题提供了一种解决方案。合成了两个系列的带有三环DNA结合部分的胺NBTI以及带有二环DNA结合部分的酰胺NBTI，并对耐甲氧西林金黄色葡萄球菌（MRSA）进行了评价。此外，这些化合物和一系列双环胺类似物显示出对敏感和耐药淋病奈瑟菌的高活性，扩展了这些二氧杂环己烷连接的NBTI的谱。
Antibacterial resistance continues its devastation of available therapies. Novel bacterial topoisomerase inhibitors (NBTIs) offer one solution to this critical issue. Two series of amine NBTIs bearing tricyclic DNA-binding moieties as well as amide NBTIs with a bicyclic DNA-binding moiety were synthesized and evaluated against methicillin-resistantStaphylococcus aureus(MRSA). Additionally, these compounds and a series of bicyclic amine analogues displayed high activity against susceptible and drug-resistantNeisseria gonorrhoeae, expanding the spectrum of these dioxane-linked NBTIs.