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Molecules 2016, 21(1), 96; doi:10.3390/molecules21010096

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

1
College of Science, Northwest A & F University, Yangling 712100, Shaanxi, China
2
Key Laboratory of Botanical Pesticide R & D in Shaanxi Province, Northwest A & 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
Received: 12 November 2015 / Revised: 30 December 2015 / Accepted: 12 January 2016 / Published: 15 January 2016
(This article belongs to the Section Medicinal Chemistry)
View Full-Text   |   Download PDF [1159 KB, uploaded 15 January 2016]   |  

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
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Dan, W.; Geng, H.; Qiao, J.; Guo, R.; Wei, S.; Li, L.; Wu, W.; Zhang, J. Efficient Synthesis and Antibacterial Evaluation of (±)-Yanglingmycin and Its Analogues. Molecules 2016, 21, 96.

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