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Antimicrobial evaluation and action mechanism of pyridinium-decorated 1,4-pentadien-3-one derivatives
Bioorganic & Medicinal Chemistry Letters ( IF 2.5 ) Pub Date : 2018-04-16 , DOI: 10.1016/j.bmcl.2018.04.034
Jian Zhou , Qing-Qing Tao , Pei-Yi Wang , Wu-Bin Shao , Zhi-Bing Wu , Zhong Li , Song Yang

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 EC50 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.



中文翻译:

吡啶鎓修饰的1,4-戊二烯-3-酮衍生物的抗菌性能及作用机理

通过将吡啶鎓阳离子的关键骨架和1,4-戊二烯-3-one骨架整合在一个分子结构中,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,某些靶分子对六种植物致病菌株具有相当大的生物活性,特别是对于米氏黄单胞菌米曲霉,最小EC 50值可以达到0.504 µg / mL。提出了这种化合物的合理作用机理,并通过荧光光谱,荧光显微镜和扫描电子显微镜进行了证实。我们预期该发现可以促进抗菌化学研究中高效铅化合物的发现。

更新日期:2018-04-16
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