- Efficient synthesis and antibacterial evaluation of (±)-Yanglingmycin and its analogues
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An efficient synthetic route was developed for the large-scale preparation of (±)-Yanglingmycin and its analogues. Three series of derivatives of (±)-Yanglingmycin were synthesized and the structures of all compounds were elucidated by analyses of NMR and ESI-MS spectra data. Moreover, their antibacterial activities against seven species of bacteria were systematically evaluated by the micro-broth dilution method, most of which displayed considerable activity. It was worth noting that compounds 5b, 5c, 5d, 6g, and 7 were found to be the most promising leading candidates, with peak MIC values of 0.98 μg.mL-1 for Bacillus subtilis, which is superior to positive controls (MIC = 3.91 μg.mL-1). The above results might lay the firm foundation for the design and synthesis of novel antibacterial drugs based on (±)-Yanglingmycin.
- Dan, Wenjia,Geng, Huiling,Qiao, Jianwen,Guo, Rui,Wei, Shaopeng,Li, Longbo,Wu, Wenjun,Zhang, Jiwen
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- A mild catalytic synthesis of 2-oxazolines: Via oxetane ring-opening: Rapid access to a diverse family of natural products
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A new catalytic protocol for the expedient synthesis of oxazolines from oxetanes is disclosed. This mild process complements the conventional oxazoline synthesis based on non-catalytic cyclization of β-hydroxy or unsaturated amides. It is also a new addition to the reactivity profile of oxetanes leading to heterocycles. In the presence of In(OTf)3, various 3-amido oxetanes underwent smooth intramolecular cyclization to form the corresponding 2-oxazolines, including some valuable oxazoline-based bidentate ligands. This protocol also provides rapid access to various natural products and antibacterial molecules.
- Huang, Hai,Yang, Wen,Chen, Zuliang,Lai, Zengwei,Sun, Jianwei
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p. 9586 - 9590
(2019/11/05)
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