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

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.

Novel Flavonol Derivatives Bearing a 1,2,3,4-Tetrahydroquinoline Moiety: Design, Synthesis, and Anti-Phytophthora capsici Activity.

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.

Novel Pyrazole-4-carboxamide Derivatives with a Tetrahydroquinoline Skeleton: Promising SDHIs for the Control of Rhizoctonia solani.

Findings suggested that compound 6m might be a potent candidate as a succinate dehydrogenase inhibitor (SDHI) against R. solani with strong protective and curative effects even at 50 μg/mL.

Synthesis and Antifungal Activities of Perillyl Alcohol Based 1,3,4‐Thiadiazole‐Thioether Compounds

ABSTRACT A series of 33 perillyl alcohol based 1,3,4‐thiadiazole‐thioether compounds were designed and synthesized through active substructure splicing. Their structures were confirmed by 1H NMR, 13C NMR, and HRMS, and their antifungal activities were evaluated in vitro. At a concentration of 50 mg/L, the target compounds exhibited varying inhibitory activities against Gibberella zeae (G. zeae), Botrytis cinerea, Rhizoctonia solani (R. solani), Rhizoctonia cerealis (R. cerealis), and Physalospora piricola (P. piricola). Among these, compound V15 (R = 3‐FC6H4) demonstrated the strongest effects against G. zeae, R. solani, R. cerealis, and P. piricola, with inhibition rates of 77.8%, 67.3%, 83.9%, and 86.1%, respectively. Notably, its activity against G. zeae (77.8%) surpassed that of the positive control chlorothalonil (73.1%), and its activity against P. piricola (86.1%) was comparable to that of chlorothalonil (89.3%). A preliminary three‐dimensional quantitative structure–activity relationship (3D‐QSAR) model for R. cerealis inhibition was established using comparative molecular field analysis (CoMFA), yielding a reliable model (r2 = 0.991, q2 = 0.547).

Design, Synthesis, and Antifungal Evaluation of Novel Formononetin-Benzothiazole Hybrids with Preliminary Mechanistic Insights.

Although the precise molecular target remains unknown, H2 shows promise as a lead candidate, and the benzothiazole moiety appears critical for enhancing activity, and the preliminary basis for developing eco-friendly fungicides is provided.

Synthesis and antifungal activity evaluation of flavonol derivatives containing an imidazolidinone moiety.