Synthesis and Antibacterial Evaluation of N-phenylacetamide Derivatives Containing 4-Arylthiazole Moieties

摘要

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.