title: Efficient Synthesis and Antibacterial Evaluation of (±)-Yanglingmycin and Its Analogues.
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.
authors.affiliation: College of Science, Northwest A &amp; F University, Yangling 712100, Shaanxi, China. dwj586@gmail.com.|Key Laboratory of Botanical Pesticide R &amp; D in Shaanxi Province, Northwest A &amp; F University, Yangling 712100, Shaanxi, China. dwj586@gmail.com.
authors.forename: Wenjia
authors.initials: W
authors.lastname: Dan
authors.affiliation: College of Science, Northwest A &amp; F University, Yangling 712100, Shaanxi, China. genghuiling5@163.com.
authors.forename: Huiling
authors.initials: H
authors.lastname: Geng
authors.affiliation: College of Science, Northwest A &amp; F University, Yangling 712100, Shaanxi, China. 18700427513@163.com.
authors.forename: Jianwen
authors.initials: J
authors.lastname: Qiao
authors.affiliation: College of Science, Northwest A &amp; F University, Yangling 712100, Shaanxi, China. 18740456637@163.com.|Key Laboratory of Botanical Pesticide R &amp; D in Shaanxi Province, Northwest A &amp; F University, Yangling 712100, Shaanxi, China. 18740456637@163.com.
authors.forename: Rui
authors.initials: R
authors.lastname: Guo
authors.affiliation: Key Laboratory of Botanical Pesticide R &amp; D in Shaanxi Province, Northwest A &amp; F University, Yangling 712100, Shaanxi, China. weishaopeng@nwsuaf.edu.cn.
authors.forename: Shaopeng
authors.initials: S
authors.lastname: Wei
authors.affiliation: College of Science, Northwest A &amp; F University, Yangling 712100, Shaanxi, China. lilongbo528@126.com.|Key Laboratory of Botanical Pesticide R &amp; D in Shaanxi Province, Northwest A &amp; F University, Yangling 712100, Shaanxi, China. lilongbo528@126.com.
authors.forename: Longbo
authors.initials: L
authors.lastname: Li
authors.affiliation: Key Laboratory of Botanical Pesticide R &amp; D in Shaanxi Province, Northwest A &amp; F University, Yangling 712100, Shaanxi, China. wuwenjun@nwsuaf.edu.cn.
authors.forename: Wenjun
authors.initials: W
authors.lastname: Wu
authors.affiliation: College of Science, Northwest A &amp; F University, Yangling 712100, Shaanxi, China. nwzjw@nwsuaf.edu.cn.|Key Laboratory of Botanical Pesticide R &amp; D in Shaanxi Province, Northwest A &amp; F University, Yangling 712100, Shaanxi, China. nwzjw@nwsuaf.edu.cn.
authors.forename: Jiwen
authors.initials: J
authors.lastname: Zhang
mesh_terms: D000900:Anti-Bacterial Agents / Q000138:chemical synthesis* / Q000494:pharmacology; D006090:Gram-Negative Bacteria / Q000187:drug effects / Q000254:growth & development; D006094:Gram-Positive Bacteria / Q000187:drug effects / Q000254:growth & development; D009682:Magnetic Resonance Spectroscopy; D008826:Microbial Sensitivity Tests; D010080:Oxazoles / Q000138:chemical synthesis* / Q000494:pharmacology; D013329:Structure-Activity Relationship; D013844:Thiazoles / Q000138:chemical synthesis* / Q000494:pharmacology
chemical_list: D000900:Anti-Bacterial Agents; D010080:Oxazoles; D013844:Thiazoles; C000602973:yanglingmycin
keywords: Yanglingmycin; analogues; antibacterial activity; synthesis