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.
Molecules. 2020 Apr 12;25(8):1772. doi: 10.3390/molecules25081772.
A series of new -phenylacetamide derivatives containing 4-arylthiazole moieties was designed and synthesized by introducing the thiazole moiety into the amide scaffold. The structures of the target compounds were confirmed by H-NMR, C-NMR and HRMS. Their in vitro antibacterial activities were evaluated against three kinds of bacteria- pv. (), pv. () and pv ()-showing promising results. The minimum 50% effective concentration (EC) value of (4-((4-(4-fluoro-phenyl)thiazol-2-yl)amino)phenyl)acetamide () is 156.7 µM, which is superior to bismerthiazol (230.5 µM) and thiodiazole copper (545.2 µM). A scanning electron microscopy (SEM) investigation has confirmed that compound could cause cell membrane rupture of . In addition, the nematicidal activity of the compounds against () was also tested, and compound displayed excellent nematicidal activity, with mortality of 100% and 53.2% at 500 μg/mL and 100 μg/mL after 24 h of treatment, respectively. The preliminary structure-activity relationship (SAR) studies of these compounds are also briefly described. These results demonstrated that phenylacetamide derivatives may be considered as potential leads in the design of antibacterial agents.
设计并合成了一系列含有 4-芳基噻唑部分的新型苯乙酰胺衍生物，通过将噻唑部分引入酰胺支架中。通过 1 H-NMR、 13 C-NMR 和 HRMS 确证了目标化合物的结构。它们对三种细菌（ pv. ()、 pv. () 和 pv. ()）的体外抗菌活性评估结果表明，这些化合物具有很好的前景。（4-((4-(4-氟苯基)噻唑-2-基)氨基)苯基)乙酰胺（）的最小 50%有效浓度（EC）值为 156.7 µM，优于双甲脒（230.5 µM）和噻二唑铜（545.2 µM）。扫描电子显微镜（SEM）研究证实，化合物 可导致 的细胞膜破裂。此外，还测试了这些化合物对 () 的杀线虫活性，化合物 表现出优异的杀线虫活性，在 500 µg/mL 和 100 µg/mL 处理 24 小时后，死亡率分别为 100%和 53.2%。还简要描述了这些化合物的初步构效关系（SAR）研究。这些结果表明，苯乙酰胺衍生物可能被认为是设计抗菌剂的潜在先导化合物。
