State Key Laboratory Breeding Base of Green Pesticide and Agricultural Bioengineering, Key Laboratory of Green Pesticide and Agricultural Bioengineering, Ministry of Education, Guizhou University, Huaxi District, Guiyang 550025, China.
State Key Laboratory Breeding Base of Green Pesticide and Agricultural Bioengineering, Key Laboratory of Green Pesticide and Agricultural Bioengineering, Ministry of Education, Guizhou University, Huaxi District, Guiyang 550025, China.
Pestic Biochem Physiol. 2018 May;147:11-19. doi: 10.1016/j.pestbp.2017.10.011. Epub 2017 Nov 8.
Various 1,3,4-oxadiazole thioether derivatives containing 2-chloro-5-methylene pyridine, 2-chloro-5-methylene thiazole, 3,4-dimethoxy-2-methylene pyridine, and N,N-dimethyl-2-ethylamino moieties were designed, synthesized, and assessed for their antibacterial activities against Xanthomonas oryzae pv. oryzae (Xoo) via the turbidimeter test in vitro. Preliminary bioassay results confirmed good antibacterial activities for most of these compounds. Among these substances, compound 6r showed the best inhibitory effect against Xoo, and its half-maximal effective concentration (EC) value is 4.78μg/mL, which is superior to that of commercial agent bismerthiazol (87.55μg/mL). We then performed a label-free quantitative proteomic analysis of the response of Xoo to 6r. A total of 1363 proteins were identified in the control and treatment groups. Upon treatment with the minimum inhibitory concentration, 349 proteins were found to be differentially expressed (fold changes>1.5, p<0.05), enriched, and may be involved in purine metabolism.
设计、合成了一系列含 2-氯-5-亚甲基吡啶、2-氯-5-亚甲基噻唑、3,4-二甲氧基-2-亚甲基吡啶和 N,N-二甲基-2-乙氨基部分的 1,3,4-噁二唑硫醚衍生物，并通过体外浊度法评估了它们对水稻白叶枯病菌（Xoo）的抗菌活性。初步生物测定结果证实，这些化合物大多数具有良好的抗菌活性。在这些物质中，化合物 6r 对 Xoo 的抑制作用最好，其半数最大有效浓度（EC）值为 4.78μg/mL，优于商业药剂双脒噻唑（87.55μg/mL）。然后，我们对 Xoo 对 6r 的反应进行了无标记定量蛋白质组学分析。在对照组和处理组中鉴定出了 1363 种蛋白质。在最低抑菌浓度下处理后，发现 349 种蛋白质表达差异（倍数变化>1.5，p<0.05），这些蛋白质可能参与嘌呤代谢。
