An efficient route to various vancoresmycin‐type tetramic acids has been developed. The modular route is based on an effective Fries‐type rearrangement to introduce various appending acetyl residues. The minimum inhibitory concentration (MIC) values of the new tetramic acids against Staphylococcus aureus and Escherichia coli were determined, revealing that three of the new compounds exhibit antimicrobial activity against S. aureus . These bioactive compounds were structurally most closely related to the authentic vancoresmycin building block. Additionally, the compounds induced a lial‐lux bioreporter, which responds to cell wall stress induced by antibiotics that interfere with the lipid II biosynthesis cycle. These data suggest the tetramic acid moiety to be a part of the vancoresmycin pharmacophore.

中文翻译：

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万古霉素衍生的四酸片段的合成对金黄色葡萄球菌具有抑制作用。

已经开发出一种有效的途径来生产各种万古霉素型四酸。模块化路线基于有效的Fries类型重排，可引入各种附加的乙酰基残基。的对新的特特拉姆酸的最小抑制浓度（MIC）值的金黄色葡萄球菌和大肠杆菌进行了测定，揭示了三个新化合物表现出抗微生物活性的金黄色葡萄球菌。这些生物活性化合物在结构上与真正的万古霉素构件密切相关。此外，该化合物引起的LIAL -勒克斯bioreporter，它对干扰脂质II生物合成周期的抗生素诱导的细胞壁应激作出反应。这些数据表明，该四酸部分是万古霉素药效团的一部分。