posted on 2024-12-12, 19:55authored byYixing Gao, Liang Chen, Dongdong Liu, Chunfeng Luo, Jialin Ye, Hongyan Pei, Jing Zhang, Lixin Zhang
Citrus canker, caused by Xanthomonas citri subsp. citri (Xcc), poses a significant
threat to citrus production worldwide. To develop effective and eco-friendly
antibacterial agents, we designed and synthesized phenyl-hydrazonomalononitrile
derivatives using a scaffold-hopping strategy. Among these, FM-568 emerged as a potent candidate, exhibiting broad-spectrum
antibacterial activity in vitro against various phytopathogenic
bacteria, including Xcc. Greenhouse experiments demonstrated
that FM-568 achieved a control efficacy of 88.36% against
citrus canker at 400 μg/mL, with an EC50 of
26.68 μg/mL. Field trials in two major citrus-producing
regions in China confirmed its effectiveness, yielding control efficacies
of 86.60 and 77.87% at 400 μg/mL, outperforming conventional
agents like zinc thiazole and thiadiazole copper. Density functional
theory calculations suggested that FM-568′s optimized
scaffold and electronic properties contribute to its enhanced antibacterial
activity. These findings indicate that FM-568 is a promising
eco-friendly alternative for managing citrus canker. Further studies
on its mechanism of action, safety profile, and formulation optimization
are warranted to advance its development for sustainable citrus production.