金融时报
稻黄单胞菌
抗菌剂
生物
微生物学
丁香假单胞菌
细菌
细菌性疫病
黄单胞菌
抗菌肽
细菌细胞结构
病菌
细菌性疾病
人类病原体
抗菌活性
假单胞菌
生物技术
公认安全
生物化学
抗菌剂
抗生素耐药性
致病菌
作者
Wan Chen,Linli Yang,Xin-Ming Yang,Pei‐Bu Yu,Jin‐Sha Yang,Xiang Zhou,Li‐Wei Liu,Zhibing Wu,Song Yang
摘要
Abstract BACKGROUND Phytopathogenic bacteria threaten global food security by reducing crop yields, degrading quality, and causing mycotoxin contamination. Therefore, there is an urgent need to develop highly effective bactericides with novel mechanisms of action. FtsZ (filamentous temperature‐sensitive protein Z) a key protein that forms the Z‐ring at the cell center to coordinate division. Although it has been recognized as an important target for novel antibacterial agents, research on its agricultural inhibitors remains relatively scarce. RESULTS Using active fragment combination strategy, we rationally designed and synthesized a series of 2‐alkenylquinolin‐1‐ium derivatives and rigorously evaluated their antimicrobial efficacy against three agriculturally devastating pathogens: Xanthomonas oryzae pv. oryzae ( Xoo ), Xanthomonas axonopodis pv. citri ( Xac ), and Pseudomonas syringae pv. actinidiae ( Psa ). Among them, compound A11 exhibited exceptional antibacterial activity against all three pathogens with half‐maximal effective concentration (EC 50 ) values of 0.024, 0.074, and 3.428 μg/mL respectively. Formulation with adjuvant fatty alcohol polyglycolether (MOA‐3) changed its physicochemical properties and improved foliar adhesion on the surface of leaves, increasing in vivo disease control efficacy from 44.82% to 55.41%. Mechanistic profiling revealed compound A11 binds to the interdomain cleft of Xoo FtsZ, inhibits Xoo FtsZ polymerization, and induced bacterial filamentation. Furthermore, compound A11 demonstrated favorable biosafety parameters with low phytotoxicity and negligible earthworm toxicity. CONCLUSION This study validates FtsZ, an evolutionarily conserved bacterial division protein, as a strategic target for antimicrobial development, and identifies compound A11 as a potent, environmentally friendly FtsZ inhibitor. Beyond providing a promising Xoo FtsZ lead compound, this work establishes a theoretical basis for bactericide design. © 2026 Society of Chemical Industry.
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