Efficient Synthesis and Antibacterial Evaluation of ±-Yanglingmycin and Its AnaloguesReport as inadecuate




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1

College of Science, Northwest A and F University, Yangling 712100, Shaanxi, China

2

Key Laboratory of Botanical Pesticide R and D in Shaanxi Province, Northwest A and F University, Yangling 712100, Shaanxi, China



These authors contributed equally to this work.





*

Author to whom correspondence should be addressed.



Academic Editor: Derek J. McPhee

Abstract 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. View Full-Text

Keywords: synthesis; Yanglingmycin; antibacterial activity; analogues synthesis; Yanglingmycin; antibacterial activity; analogues





Author: Wenjia Dan 1,2,†, Huiling Geng 1,†, Jianwen Qiao 1, Rui Guo 1,2, Shaopeng Wei 2, Longbo Li 1,2, Wenjun Wu 2 and Jiwen Zhang 1,2,*

Source: http://mdpi.com/



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