Resistance to single-target fungicides necessitates structurally innovative antifungal agents with broadened modes of action. Herein, a series of pyrazole-oxadiazole-linked 1,2,4-triazole derivatives (L1-L39) were designed and synthesized via molecular hybridization. Compound L22 exhibited exceptional activity against Magnaporthe grisea (EC50 = 5.96 μg/mL), outperforming the commercial fungicide isoprothiolane, and potently inhibited Botrytis cinerea and Verticillium dahliae. In vivo assays confirmed its excellent protective and curative efficacies against rice blast. Mechanistic investigations revealed that L22 induces severe cellular disruption, characterized by compromised membrane integrity, cell wall deformation, and broad dysregulation of sterol/lipid metabolism, carbohydrate utilization, mitochondrial respiration, and stress-response pathways. Furthermore, L22 displayed no detectable phytotoxicity toward rice seedlings at effective concentrations. These findings establish pyrazole-oxadiazole-triazole derivatives as potent, safe, and mechanistically distinct antifungal leads, warranting further development for agricultural disease management.
Fa-li Wang, Xiao-li Ren, Lin Gao et al.· Journal of Agricultural and...· 0 citations
A series of thiazolidinedione derivatives containing thioamide and piperidine moieties were designed, synthesized, and evaluated for antifungal activity against plant pathogenic fungi. Several compounds exhibited potent antifungal activity, among which Z17 was the most active against Rhizoctonia solani (EC50 = 1.8 μg/mL), with substantially greater activity than azoxystrobin (Az; EC50 = 42.6 μg/mL). Physiological analyses indicated that Z17 disrupted membrane integrity and cellular energy metabolism, as reflected by increased malondialdehyde levels and decreased pyruvate kinase activity and pyruvate content. Density functional theory calculations, molecular docking, and molecular dynamics simulations suggested that Z17 forms favorable interactions with the cytochrome bc1 complex. Preliminary safety assessments showed no significant effects on rice seed germination or earthworm viability. These findings suggest Z17 as a promising lead for the development of antifungal agents against crop pathogens.
Junrong Song, Shuang Feng, Miaohe Zhang et al.· Journal of Agricultural and...· 0 citations
Mechanistic studies revealed that Q8 disrupted cell membrane integrity and inhibited succinate dehydrogenase (SDH) activity, with computational simulations suggesting a higher binding affinity for SDH than fluopyram.
Qingxue Hu, Xiaoting Geng, Fang Tian et al.· Journal of Agricultural and...· 0 citations
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