Design, synthesis and biological activities of 1,2,4‐triazolo[1,5‐a]pyrimidine‐7‐amine derivatives bearing 1,2,4‐oxadiazole motif

Journal of Heterocyclic Chemistry, Год журнала: 2022, Номер 60(2), С. 241 - 251

Опубликована: Сен. 9, 2022

Abstract Pyrimidine is an important heterocyclic ring with various activities, which are widely used in the field of pesticides and medicines. In this paper, a series 1,2,4‐triazolo[1,5‐ ]pyrimidine‐7‐amine compounds ( V1 – V16 ) containing 1,2,4‐oxadiazole moiety were designed synthesized. Their structures confirmed by 1 H NMR, 13 C 19 F HRMS. The biological activity results showed that V5 , V6 V7 V9 V10 V12 V13 possessed good against Mythimna separate at 500 ppm, while compound V4 exhibited moderate Aphis medicagini ppm. Furthermore, V3 displayed fungicidal Pseudoperonospora cubensis 200

Язык: Английский

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Advancement of Phenoxypyridine as an Active Scaffold for Pesticides

Molecules, Год журнала: 2022, Номер 27(20), С. 6803 - 6803

Опубликована: Окт. 11, 2022

Phenoxypyridine, the bioisostere of diaryl ethers, has been widely introduced into bioactive molecules as an active scaffold, which different properties from ethers. In this paper, bioactivities, structure-activity relationships, and mechanism compounds containing phenoxypyridine were summarized, may help to explore lead discover novel pesticides with potential bioactivities.

Язык: Английский

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Synthesis, Structure, and Antifungal Activities of 3-(Difluoromethyl)-Pyrazole-4-Carboxylic Oxime Ester Derivatives

Heteroatom Chemistry, Год журнала: 2022, Номер 2022, С. 1 - 8

Опубликована: Авг. 28, 2022

Fifteen new pyrazole-4-carboxylic oxime ester derivatives were conveniently synthesized, and their structures confirmed by 1H NMR, 13C HRMS, X-ray diffraction. Antifungal assays indicated that some of these compounds possessed good activity against S. sclerotiorum, B. cinerea, R. solani, P. oryae, piricola at 50 ppm. Structure-activity relationships (SAR) studied molecular docking simulation.

Язык: Английский

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Synthesis, Antifungal Activity, and Molecular Docking Study of Novel 3‐Carene‐Derived 4‐Substituted Phenyl‐1,2,4‐Triazolinthiones Bearing gem‐Dimethylcyclopropane Moiety

Chemistry & Biodiversity, Год журнала: 2022, Номер 19(11)

Опубликована: Сен. 19, 2022

Abstract For exploring new natural product‐based leading compounds with antifungal activity, 15 novel 3‐carene‐derived 4‐substituted phenyl‐1,2,4‐triazolinthiones 7a ∼ 7o bearing gem ‐dimethylcyclopropane moiety were synthesized and structurally characterized by UV/VIS, FT‐IR, 1 H‐NMR, 13 C‐NMR, ESI‐MS elemental analysis. The preliminary bioassay at 50 μg/mL showed that all of the target exhibited certain in vitro inhibitory activities against eight tested fungi, which compound 7g (R= m , p‐ Cl) displayed better inhibition activity (85.0 %) P. piricola than positive control Chlorothalonil. Furthermore, a reasonable effective 3D structure phytofungal CYP51 was constructed homology modeling. Molecular docking study revealed total scores higher Prothioconazole. In addition, it found could readily embed into binding site, therein shared similar interactions case Thus, deserved further as an compound.

Язык: Английский

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Synthesis and pesticidal activity of new 1,3,4-oxadiazole thioether compounds containing a trifluoromethylpyrazoyl moiety

Research on Chemical Intermediates, Год журнала: 2022, Номер 48(11), С. 4753 - 4767

Опубликована: Сен. 20, 2022

Язык: Английский

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