Design, Synthesis, Antibacterial Activity, and Mechanisms of Novel Benzofuran Derivatives Containing Disulfide Moieties.

The unsatisfactory effects of conventional bactericides and antimicrobial resistance have increased the challenges in managing plant diseases caused by bacterial pests. Here, we report the successful design and synthesis of benzofuran derivatives using benzofuran as the core skeleton and splicing the disulfide moieties commonly seen in natural substances with antibacterial properties. Most of our developed benzofurans displayed remarkable antibacterial activities to frequently encountered pathogens, including pv (), pv (), and pv (). With the assistance of the three-dimensional quantitative constitutive relationship (3D-QSAR) model, the optimal compound was obtained, which has better in vitro antibacterial activity with EC values of 0.28, 0.56, and 10.43 μg/mL against , , and , respectively, than those of positive control, TC (66.41, 78.49, and 120.36 μg/mL) and allicin (8.40, 28.22, and 88.04 μg/mL). Combining the results of proteomic analysis and enzyme activity assay allows the antibacterial mechanism of to be preliminarily revealed, suggesting its potential as a versatile bactericide in combating bacterial pests in the future.