Zhou Jian, Tao Qing-Qing, Wang Pei-Yi, Shao Wu-Bin, Wu Zhi-Bing, Li Zhong, Yang Song
State Key Laboratory Breeding Base of Green Pesticide and Agricultural Bioengineering, Key Laboratory of Green Pesticide and Agricultural Bioengineering, Ministry of Education, Center for R&D of Fine Chemicals of Guizhou University, 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, Center for R&D of Fine Chemicals of Guizhou University, Guiyang 550025, China.
Bioorg Med Chem Lett. 2018 Jun 1;28(10):1742-1746. doi: 10.1016/j.bmcl.2018.04.034. Epub 2018 Apr 16.
A type of pyridinium-decorated 1,4-pentadien-3-one derivatives possessing flexible alkyls were designed and synthesized by integrating the key scaffolds of pyridinium cations and 1,4-pentadien-3-one skeleton in a single molecular architecture. Antimicrobial bioassays indicated that some of the target molecules exerted considerable bioactivities against six phytopathogenic strains, especially for Xanthomonas oryzae pv. oryzae, the minimal EC value can reach to 0.504 µg/mL. A plausible action mechanism for this kind of compounds was proposed and confirmed by employing fluorescent spectroscopy, fluorescence microscopy, and scanning electron microscopy. We anticipated that this finding can promote high-efficient lead compounds discovery in the research of antimicrobial chemotherapy.
通过将吡啶鎓阳离子和1,4 - 戊二烯 - 3 - 酮骨架的关键支架整合到单一分子结构中，设计并合成了一种具有柔性烷基的吡啶鎓修饰的1,4 - 戊二烯 - 3 - 酮衍生物。抗菌生物测定表明，一些目标分子对六种植物病原菌株具有相当大的生物活性，特别是对水稻白叶枯病菌，最小EC值可达0.504μg/mL。通过荧光光谱、荧光显微镜和扫描电子显微镜提出并证实了这类化合物的一种合理作用机制。我们预计这一发现能够促进抗菌化疗研究中高效先导化合物的发现。
