Pest management science · 2026
Design, synthesis, and biological evaluation of a novel library of indole-benzoxazole derivatives as potential antifungal and antibacterial agents.
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Zou Hongqian, Cheng Ziye, Pu Haotao, Tian Fang, Sun Mingman, Yang Ying, Xing Lang, Kandegama Wasala Mudiyanselage Wishwajith Wickramabahu, Gu Lijun, Xue Wei
Аннотация
BACKGROUND: Plant diseases threaten global agriculture. A series of 22 novel indole-benzoxazole derivatives were synthesized to evaluate their antimicrobial potential against eight plant pathogenic fungi and three bacteria.
RESULTS: Several compounds exhibited potent antimicrobial activity. Specifically, C12 showed high efficacy against Phomopsis sp. (EC₅₀ = 5.1 μg mL-1 vs azoxystrobin 44.7 μg mL-1) and Rhizoctonia solani (EC₅₀ = 7.9 μg mL-1 vs 17.3 μg mL-1). C4 strongly inhibited Xanthomonas axonopodis pv. citri (EC₅₀ = 8.5 μg mL-1 vs thiodiazole copper 73.3 μg mL-1). In vivo assays confirmed their superior curative and protective efficacy. Mechanistic studies revealed that C12 acted by disrupting cell wall/membrane integrity, while C4 functioned by suppressing biofilm formation and reducing extracellular polysaccharide production.
CONCLUSION: C12 and C4 demonstrate promising antimicrobial potential through distinct action mechanisms, providing valuable candidates for the development of new plant disease control agents. © 2026 Society of Chemical Industry.
RESULTS: Several compounds exhibited potent antimicrobial activity. Specifically, C12 showed high efficacy against Phomopsis sp. (EC₅₀ = 5.1 μg mL-1 vs azoxystrobin 44.7 μg mL-1) and Rhizoctonia solani (EC₅₀ = 7.9 μg mL-1 vs 17.3 μg mL-1). C4 strongly inhibited Xanthomonas axonopodis pv. citri (EC₅₀ = 8.5 μg mL-1 vs thiodiazole copper 73.3 μg mL-1). In vivo assays confirmed their superior curative and protective efficacy. Mechanistic studies revealed that C12 acted by disrupting cell wall/membrane integrity, while C4 functioned by suppressing biofilm formation and reducing extracellular polysaccharide production.
CONCLUSION: C12 and C4 demonstrate promising antimicrobial potential through distinct action mechanisms, providing valuable candidates for the development of new plant disease control agents. © 2026 Society of Chemical Industry.