含 5-硝基呋喃的新型甲氧基丙烯酸酯衍生物合成及抗菌活性

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引用格式:,等. 含5-硝基呋喃的新型甲氧基丙烯酸酯衍生物合成及抗菌活性[J]. 当代化工,2026,55(4):776-782.

LIU Min, CHEN Biao, YU Siying, et al. Synthesis and Antibacterial Activity of Novel Methoxyacrylate Derivatives Containing a 5-Nitrofuran Moiety[J]. Contemporary Chemical Industry, 2026, 55(4): 776-782.

余思颖,刘济,柴慧芳

中图分类号:TQ455.4

文献标志码:A

文章编号:1671-0460(2026)04-0776-07

Synthesis and Antibacterial Activity of Novel Methoxyacrylate Derivatives Containing a 5-Nitrofuran Moiety

LIU Min, CHEN Biao, YU Siying, LIU Ji, CHAI Huifang

(School of Pharmacy, Guizhou University of Traditional Chinese Medicine, Guiyang Guizhou , China)

Abstract: To develop novel methoxyacrylate fungicides with high activity, using o-methylphenylacetic acid as the starting material, six novel strobilurin derivatives containing a nitrofuran moiety were designed and synthesized via reactions including esterification and nucleophilic addition-elimination. Their antifungal activities against five plant pathogenic fungi were evaluated in vitro, and molecular docking was used to investigate the binding mode of highly active compounds with cytochrome b (cyt b). The results showed that at mass concentration of 50 μ g ⋅ mL -1 , compound G 2 exhibited potent inhibitory activity against Alternaria solani, Gibberella zeae, and Botryosphaeria dothidea, with inhibition rates of 75.0%, 58.2%, and 63.1%, respectively. Its EC 50 against A. solani was 0.07 μ g ⋅ mL -1 , comparable to kresoxim-methyl (0.06 μ g ⋅ mL -1 ) and azoxystrobin (0.04 μ g ⋅ mL -1 ). The binding energy of compound G 2 to cyt b was -40.75 kJ ⋅ mol -1 , and its binding affinity was superior to that of kresoxim-methyl (-38.66 kJ ⋅ mol -1 ).

Keywords: Methoxyacrylate; 5-Nitro-2-substituted furan; Design; Synthesis; Antifungal activity; Molecular docking

当前,农药领域正面临传统产品作用模式单一导致抗药性加剧以及环境与农药残留问题的双重挑战[1-3]。(剩余15530字)

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