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Efficient Synthesis and Antibacterial Evaluation of (±)-Yanglingmycin and Its Analogues

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 antibac...

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Detalles Bibliográficos
Autores principales: Dan, Wenjia, Geng, Huiling, Qiao, Jianwen, Guo, Rui, Wei, Shaopeng, Li, Longbo, Wu, Wenjun, Zhang, Jiwen
Formato: Online Artículo Texto
Lenguaje:English
Publicado: MDPI 2016
Materias:
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6273348/
https://www.ncbi.nlm.nih.gov/pubmed/26784161
http://dx.doi.org/10.3390/molecules21010096
Descripción
Sumario: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.