Wang Pei-Yi, Fang He-Shu, Shao Wu-Bin, Zhou Jian, Chen Zhuo, Song Bao-An, 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. 2017 Sep 15;27(18):4294-4297. doi: 10.1016/j.bmcl.2017.08.040. Epub 2017 Aug 19.
Various pyridinium-functionalized carbazole derivatives were constructed by coupling the key fragments of carbazole skeleton and pyridinium nucleus in a single molecular architecture. Antibacterial bioassays revealed that some of the title compounds displayed impressive bioactivities against plant pathogens such as Xanthomonas oryzae pv. oryzae, Ralstonia solanacearum, and Xanthomonas axonopodis pv. citri with minimal EC values of up to 0.4, 0.3, and 0.3mg/L, respectively. These bioactivities were achieved by systematically tuning and optimizing bridging linker, alkyl length of the tailor, and substituents on the carbazole scaffold. Compared with the bioactivity of the lead compound (AP-10), antibacterial efficacy dramatically increased by approximately 13-, 104- and 21-fold. This finding suggested that these compounds can serve as new lead compounds in research on antibacterial chemotherapy.
通过在单一分子结构中偶联咔唑骨架和吡啶鎓核的关键片段，构建了各种吡啶鎓功能化咔唑衍生物。抗菌生物测定表明，一些标题化合物对水稻白叶枯病菌、青枯雷尔氏菌和柑橘溃疡病菌等植物病原体表现出令人印象深刻的生物活性，其最低有效浓度（EC）值分别高达0.4、0.3和0.3mg/L。这些生物活性是通过系统地调节和优化桥连连接基、定制的烷基长度以及咔唑支架上的取代基来实现的。与先导化合物（AP-10）的生物活性相比，抗菌效果显著提高了约13倍、104倍和21倍。这一发现表明，这些化合物可作为抗菌化疗研究中的新型先导化合物。
