华南农业大学学报2017，Vol.38Issue(3)：21-25,5.DOI:10.7671/j.issn.1001-411X.2017.03.004
取代基团对含噻二唑片段截短侧耳素衍生物抑制鸡毒支原体活性的影响
Influence of substituent groups on the antibacterial effect of pleuromutilin derivatives with thiadiazole moiety against Mycoplasma gallisepticum
摘要
Abstract
[Objective] To provide experimental data for the research and development of new antibacterials against Mycoplasma gallisepticum.[Method]Eighteen analogues of pleuromutilin possessing thiadiazole moieties at the C14 chains were synthesized.High resolution mass spectrometry was used to verify the structures of the synthesized compounds.Influence of substituted benzene on the antibacterial effects of these pleuromutilin derivatives against M.gallisepticum were investigated by in vitro drug sensitivity tests.[Result]The obtained MIC values revealed that analogues 12, 15 and 17 exhibited potential antibacterial activities against M.gallisepticum S6 strain with MIC of 0.125 0 μg·mL-1.Analogue 18 and Tiamulin (control) showed the most potent antibacterial activities against S6 strain in vitro with MIC of 0.015 6 μg·mL-1.Analogue 17, which was the product from benzoylation of the amino group of analogue 18, had lower antibacterial activity compared with analogue 18.[Conclusion] Analogue 18 can be used as a candidate compound for further development of antibacterials against M.gallisepticum.关键词
鸡毒支原体/截短侧耳素衍生物/噻二唑/高分辨质谱/最小抑菌质量浓度Key words
Mycoplasma gallisepticum/pleuromutilin derivative/thiadiazole moiety/high resolution mass spectrometry/minimum inhibitory concentration (MIC)分类
农业科技引用本文复制引用
方茜,王文湘,高美龄,阳涛,刘雅红,汤有志..取代基团对含噻二唑片段截短侧耳素衍生物抑制鸡毒支原体活性的影响[J].华南农业大学学报,2017,38(3):21-25,5.基金项目
广东省自然科学基金(S2012030006590) （S2012030006590）
广州市珠江科技新星专项(2014J2200042) （2014J2200042）
