Novel bacterial type II topoisomerase inhibitors (NBTIs) constitute a promising new class of antibacterial agents. We report a series of NBTIs with potent anti-staphylococcal activity and diminished hERG inhibition. Dioxane-linked compound 9 demonstrated MICs ≤1 μg/mL against both methicillin-susceptible (MSSA) and -resistant Staphylococcus aureus (MRSA), accompanied by reduced hERG inhibition as compared to cyclohexane- or piperidine-linked analogs.

中文翻译：

---

具有5-氨基-1,3-二恶烷接头部分的新型细菌拓扑异构酶抑制剂的合成和抗葡萄球菌活性

新型细菌II型拓扑异构酶抑制剂（NBTI）构成了有前途的新型抗菌剂。我们报告了一系列的NBTIs具有有效的抗葡萄球菌活性和减少hERG抑制作用。与环己烷或哌啶连接的类似物相比，二恶烷连接的化合物9表现出对甲氧西林敏感（MSSA）和抗性金黄色葡萄球菌（MRSA）的MIC≤1μg/ mL ，并伴随hERG抑制作用的降低。