Design and synthesis of camphor‐thiazole derivatives as potent antifungal agents: structure–activity relationship and preliminary mechanistic study DOI
Peng Dai,

Zihua Ma,

Yanan Dang

et al.

Pest Management Science, Journal Year: 2024, Volume and Issue: unknown

Published: Nov. 26, 2024

Plant pathogenic fungi pose a severe threat to crop yield and food security. This study aims investigate the potential antifungal activity mechanism of action camphor-thiazole derivatives against six plant fungi. A novel series were designed, synthesized evaluated for their effects Rhizoctonia solani, Fusarium graminearum, Valsa mali, Alternaria Colletotrichum orbiculare Botryitis cinerea.

Language: Английский

Preparation of Cinnamomum camphora essential oil microcapsules using gelatin/gum arabic and evaluation of their antifungal effects on Fusarium spp. DOI
Zaizhi Liu,

Yanting Dai,

Cheng Wei

et al.

International Journal of Biological Macromolecules, Journal Year: 2025, Volume and Issue: 303, P. 140706 - 140706

Published: Feb. 5, 2025

Language: Английский

Citations

0
Discovery of Novel Quinazolinone-2-carbohydrazide Derivatives as Effective Succinate Dehydrogenase Inhibitors and Biosafety Assessment on Rice and Zebrafish DOI

Taisen Yan,

Hong Li, Sha Li

et al.

Journal of Agricultural and Food Chemistry, Journal Year: 2025, Volume and Issue: 73(9), P. 5054 - 5066

Published: Feb. 18, 2025

To develop potent and safe antifungal agents in agriculture, a total of 48 novel quinazolinone-2-carbohydrazide derivatives were designed synthesized based on the pharmacophore hybridization method. The bioassay results demonstrated that many compounds exhibited powerful broad-spectrum inhibition activities vitro against tested fungi. For instance, E23 F23 possessed EC50 (half-maximal effective concentration) values 0.41 0.47 μg/mL Rhizoctonia solani, comparable to commercial fungicide Boscalid (EC50 = 0.49 μg/mL). Additionally, compound also pronounced effects Verticillium dahliae, Alternaria Colletotrichum gloeosporioides with 0.27, 1.15, 0.27 μg/mL, respectively. In vivo assays rice plants revealed this at 200 nearly equipotent curative protective R. as compared positive controls Carbendazim. Moreover, had an obvious activity fungal succinate dehydrogenase (SDH) from solani half-maximal concentration (IC50) 11.76 μM, interactions between SDH enzyme further confirmed by molecular docking studies. Furthermore, presence triggered morphological changes mycelia increased conductivity permeability cell membranes. Interestingly, built three-dimensional quantitative structure-activity relationship (3D-QSAR) models showed electrostatic effect played more important role maintaining anti-R. target than other effects. Finally, biosafety assessment its safety toward zebrafish.

Language: Английский

Citations

0
Novel Design of Pyrazolyl-Containing Monoterpene Compounds to Enhance Antifungal Efficacy Against Rhizoctonia solani DOI
Haowen Huang, Cong Huang,

Qingwen Fang

et al.

Journal of Agricultural and Food Chemistry, Journal Year: 2025, Volume and Issue: unknown

Published: March 17, 2025

In the fields of agriculture and forestry, there are major unknown risks associated with toxicity chemical pesticide residues pathogen resistance. To address this issue, in study, 52 novel pyrazole monoterpene compounds were obtained by organic synthesis highly active natural products evaluated for their vitro vivo antifungal activities crystal structure analysis compound 5b. The results showed that 4g 8f exhibited remarkable against Rhizoctonia solani, corresponding EC50 values reaching 4.27 4.81 mg/L. At same time, experiments both had good control effects rice sheath blight. activity these was preliminarily explored scanning electron microscopy, molecular docking, enzyme determination, cytotoxicity, indicating have potential development into low-toxic drugs.

Language: Английский

Citations

0
Target-induced dissociation of AIE metal-organic framework for fluorescence-enhanced determination of the chlorpyrifos bioaccumulation in wheat by employing Mn (III) as the active center DOI
Jie Tang,

Tingting Cai,

Na Li

et al.

Journal of Hazardous Materials, Journal Year: 2025, Volume and Issue: unknown, P. 137964 - 137964

Published: March 1, 2025

Language: Английский

Citations

0
Rational design and discovery of novel hydrazide derivatives as potent succinate dehydrogenase inhibitors inspired by natural d/l‐camphor DOI
Peng Dai,

Zihua Ma,

Guangfu Yi

et al.

Pest Management Science, Journal Year: 2024, Volume and Issue: unknown

Published: Oct. 18, 2024

Abstract BACKGROUND Succinate dehydrogenase inhibitors (SDHIs) have rapidly become one of the fastest‐growing categories fungicides used against plant pathogenic fungi. Recent research advancements emphasized that structural modifications SDHIs using naturally sourced scaffolds represent an innovative strategy for developing new, highly effective, broad‐spectrum fungicides. A novel series d/l ‐camphorhydrazide derivatives potentially targeting fungal succinate (SDH) were designed, synthesized and evaluated their antifungal effects Rhizoctonia solani , Fusarium graminearum Valsa mali Botrytis cinerea . RESULTS Amongst them, compounds A1‐7 ( d ‐camphor) A2‐7 l displayed excellent in vitro activity R. with median effective concentration (EC 50 ) values 0.38 0.48 μg mL −1 which obviously superior to boscalid (0.87 ). A2‐5 ‐camphor, EC = 3.27 exhibited good V. (2.13 − 1), A2‐21 (5.2 A1‐5 (5.15 showed F. below (5.85 Preliminary mechanistic studies, scanning transmission electron microscopy, indicated compound induced disordered entanglement hyphae, shrinkage hyphal surfaces, vacuole swelling rupture, disrupted normal growth. Additionally, production accumulation reactive oxygen species, mitochondrial membrane potential, effectively inhibited germination formation sclerotia Moreover, molecular docking results SDH enzyme assays yielded promising outcomes. CONCLUSION In this study, designed optimized emerged as candidates SDH‐targeting fungicides, demonstrating strong activity. These hold potential new agents further research. © 2024 Society Chemical Industry.

Language: Английский

Citations

1
Synthesis, antifungal activity, and 3D-QSAR study of novel L-carvone-based thiazole-hydrazone derivatives DOI
Baoyu Li,

Rongzhu Wen,

Wengui Duan

et al.

Phytochemistry Letters, Journal Year: 2024, Volume and Issue: 65, P. 58 - 63

Published: Dec. 5, 2024

Language: Английский

Citations

1
Discovery of Novel D/L-Camphor Derivatives Containing Oxime Ester as Fungicide Candidates: Antifungal Activity, Structure-Activity Relationship and Preliminary Mechanistic Study DOI
Peng Dai,

Zihua Ma,

Huizhen Xue

et al.

Published: Jan. 1, 2024

Language: Английский

Citations

0
Discovery of Novel D/L-Camphor Derivatives Containing Oxime Ester as Fungicide Candidates: Antifungal Activity, Structure-Activity Relationship and Preliminary Mechanistic Study DOI Creative Commons
Peng Dai,

Zihua Ma,

Huizhen Xue

et al.

Advanced Agrochem, Journal Year: 2024, Volume and Issue: unknown

Published: Nov. 1, 2024

Language: Английский

Citations

0
Design and synthesis of camphor‐thiazole derivatives as potent antifungal agents: structure–activity relationship and preliminary mechanistic study DOI
Peng Dai,

Zihua Ma,

Yanan Dang

et al.

Pest Management Science, Journal Year: 2024, Volume and Issue: unknown

Published: Nov. 26, 2024

Plant pathogenic fungi pose a severe threat to crop yield and food security. This study aims investigate the potential antifungal activity mechanism of action camphor-thiazole derivatives against six plant fungi. A novel series were designed, synthesized evaluated for their effects Rhizoctonia solani, Fusarium graminearum, Valsa mali, Alternaria Colletotrichum orbiculare Botryitis cinerea.

Language: Английский

Citations

0