Novel pyrazole-4-carboxamides and aromatic carboxamides derivatives containing a hydrazine moiety as potential SDHIs

Journal of Molecular Structure, Год журнала: 2023, Номер 1292, С. 136202 - 136202

Опубликована: Июль 13, 2023

Язык: Английский

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Discovery of a novel series of phenylthiazole thioether (sulfone) compounds based on natural thiasporine A as potential candidates for controlling rice fungal and bacterial diseases

Food and Energy Security, Год журнала: 2024, Номер 13(4)

Опубликована: Июль 1, 2024

Abstract Half of the world's population depends on rice for their calories. Protecting in growth period from damage caused by phytopathogens is faced with a great challenge under frequent extreme climate. To find novel fungicides to control diseases, 35 phenylthiazole‐1,3,4‐oxadiazole‐thioether (sulfone) derivatives were synthesized and evaluated efficacy against destructive fungal bacterial diseases rice. Bioassay results demonstrated that most G‐series compounds possessed excellent antifungal antibacterial activities. In particular, G1 (EC 50 = 2.22 μg/mL, R.s ) G7 2.76 showed promising activities vitro exhibited superior protective curative sheath blight vivo compared commercial carbendazim. Surprisingly, compound G2 remarkable activity Xanthomonas oryzae pv. ( Xoo an EC value 1.98 (88.08%) than thiodiazole copper (79.39%) leaf at 200 μg/mL. The abovementioned fully manifested phenylthiazole‐1,3,4‐oxadiazole‐sulfone structure, especially , had potential develop as agents controlling diseases.

Язык: Английский

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Discovery, Optimization, and Biological Evaluation of Novel Pyrazol-5-yl-phenoxybenzamide Derivatives as Potent Succinate Dehydrogenase Inhibitors

Journal of Agricultural and Food Chemistry, Год журнала: 2024, Номер 72(31), С. 17608 - 17616

Опубликована: Июль 24, 2024

The diphenyl ether molecular pharmacophore has played a significant role in the development of fungicidal compounds. In this study, variety pyrazol-5-yl-phenoxybenzamide derivatives were synthesized and evaluated for their potential to act as succinate dehydrogenase inhibitors (SDHIs). bioassay results indicate certain compounds display remarkable broad-spectrum antifungal activities. Notably, compound 12x exhibited vitro activities against Valsa mali, Gaeumannomyces graminis, Botrytis cinerea, with EC50 values 0.52, 1.46, 3.42 mg/L, respectively. These lower or comparable those Fluxapyroxad (EC50 = 12.5, 1.93, 8.33 respectively). Additionally, showed promising Sclerotinia sclerotiorum 0.82 mg/L) Rhizoctonia solani 1.86 mg/L), albeit than 0.23 0.62 mg/L). Further vivo experiments demonstrated possess effective protective V. mali S. at concentration 100 inhibition rates 66.7 89.3%, comparison, 29.2 96.4% sclerotiorum, Molecular docking analysis revealed that interacts SDH through hydrogen bonding, π-cation, π–π interactions, providing insights into probable mechanism action. Furthermore, greater binding energy enzyme inhibitory activity (ΔGcal −46.8 kcal/mol, IC50 1.22 compared ΔGcal −41.1 8.32 Collectively, our suggest could serve lead more potent SDHIs crop protection.

Язык: Английский

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Synthesis and Evaluation of Novel 1-Methyl-1H-pyrazol-5-amine Derivatives with Disulfide Moieties as Potential Antimicrobial Agents

Journal of Agricultural and Food Chemistry, Год журнала: 2024, Номер 72(37), С. 20658 - 20669

Опубликована: Сен. 3, 2024

Sulfur-containing compounds have diverse biological functions and are crucial in crop protection chemistry. In this study, a series of novel 1-methyl-1

Язык: Английский

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The discovery of 3-fluoroalkyl indoles as potential antifungal agents to control tomato gray mold caused by Botrytis cinerea

Phytochemistry Letters, Год журнала: 2023, Номер 55, С. 175 - 183

Опубликована: Июнь 1, 2023

Язык: Английский

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