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Sponsored Artificial Intelligence: A Modern Approach, Global Edition Artificial Intelligence: A Modern Approach, Global Edition

Author

Zhi-Qing Ma

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Aug 2026

Heterocycle-Substituted α-Methylene-γ-Butyrolactone Derivatives: Design, Synthesis, and Bioactivity against Phytopathogenic Fungi and Bacteria.

A series of 37 heterocycle-substituted α-methylene-γ-butyrolactone (MBL) derivatives were designed and synthesized. Bioassays showed that these derivatives possessed prominent fungicidal and bactericidal activities against Phytophthora capsici and Pseudomonas syringae pv actinidiae (Psa). Compound A6 exhibited the strongest antioomycete activity against P. capsici with an EC50 of 1.24 mg/L, presenting excellent in vivo protective (83.2%) and curative (81.2%) efficacies, while compound B12 exerted potent antibacterial activity against Psa (EC50 = 12.07 mg/L) with 72.3% protective efficacy against kiwifruit bacterial canker. Mechanistically, compound A6 functions mainly by binding to respiratory chain complex III. Notably, compound A6 caused no obvious adverse effects on chili pepper seed germination and plant growth at the tested concentrations of 100-400 mg/L. This study offers a basis for developing novel heterocycle-substituted MBL-derived agricultural antimicrobial agents.

Deyou Yang, Heng Li, Yong-Xin Liang et al. · 0 citations
Aug 2026

Design, Synthesis, and Fungicidal Activity of Novel α-Methylene-γ-Butyrolactone Derivatives Bearing Benzofuran-2-yl Moiety.

A series of 30 novel α-methylene-γ-butyrolactone (MBL) derivatives were designed and synthesized. Bioassays revealed that several compounds exhibited potent fungicidal activities against Valsa mali, Rhizoctonia solani, and Phytophthora capsici. A25 showed the highest activity against V. mali (EC50 = 0.70 mg/L). Against R. solani, A5 (EC50 = 0.94 mg/L) and A21 (EC50 = 0.69 mg/L) were highly active. Against P. capsici, A14 (EC50 = 0.69 mg/L), A21 (EC50 = 0.59 mg/L), and A24 (EC50 = 0.71 mg/L) displayed potent antioomycete activity. At 200 mg/L, A21 provided protective (88.9%) and curative (67.0%) effects in potted rice against R. solani as well as protective (91.0%) and curative (85.4%) effects on pepper plants against P. capsici. Mechanistic studies indicated that A21 blocks ATP synthesis and impairs energy metabolism. Toxicity assessment showed that A21 was nontoxic to earthworms and silkworms at the tested concentrations. This work provides insights for developing MBL derivatives as potential fungicides.

Deyou Yang, Heng Li, Jiaying Xu et al. · 0 citations

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