Agricultural production is seriously threatened by plant pathogens. The development of new fungicides with high efficacy and low toxicity urgently needed. In this study, a series pyrazole carboxamide thiazole derivatives were designed, synthesized, evaluated for their antifungal activities against nine pathogens in vitro. Bioassay results showed that most compounds (3i, 5i, 6i, 7i, 9i, 12i, 16i, 19i, 23i) exhibited good Valsa mali. particular, 6i 19i better mali EC50 values 1.77 1.97 mg/L,...

In our pursuit of novel succinate dehydrogenase inhibitor (SDHI) fungicides for agriculture, we replaced the traditional amide structure with a sulfonamide framework and introduced various heterocyclic aromatic rings at sulfonamide's termini. This strategy yielded 30 synthesized compounds, which were screened antifungal activity against eight phytopathogenic fungi. The biological assay results demonstrated that several target compounds exhibited significant in vitro activity. Notably,...

Inspired by commercially established fluxapyroxad as the lead compound of novel efficient antifungal ingredients, pyrazole carboxylate derivatives containing a flexible thiazole backbone were successfully designed, synthesized, and detected for their in vitro vivo biological activities against eight agricultural fungi. The bioassay results showed that 24 revealed excellent bioactivities Botrytis cinerea Sclerotinia sclerotiorum, with median effective concentrations (EC50) 0.40 3.54 mg/L,...

To promote the development of novel agricultural succinate dehydrogenase inhibitor (SDHI) fungicides, we introduced cinnamamide and nicotinamide structural fragments into structure pyrazol-5-yl-amide by carbon chain extension scaffold hopping, respectively, synthesized a series derivatives. The results biological activity assays indicated that most target compounds exhibited varying degrees inhibitory against tested fungi. Notably, G22, G28, G34, G38, G39 excellent in vitro antifungal...

A series of pyrazol-5-yl-benzamide derivatives containing the oxazole group were designed and synthesized as potential SDH inhibitors. According to results bioassays, most target compounds displayed moderate-to-excellent in vitro antifungal activities against Valsa mali, Sclerotinia scleotiorum, Alternaria alternata, Botrytis cinerea. Among them, C13, C14, C16 exhibited more excellently inhibitory S. sclerotiorum than boscalid (EC50 = 0.96 mg/L), with EC50 values 0.69, 0.26, 0.95 mg/L,...

Abstract BACKGROUND Succinate dehydrogenase ( SDH ) plays an important role in the Krebs cycle, which is considered as attractive target for development of succinate inhibitors SDHIs based on antifungal agents. Thus, order to discover novel molecules with high activities, a series nicotinamide derivatives bearing substituted pyrazole moieties were designed and synthesised via one‐pot reaction. RESULTS The biological assay data showed that compound 3 l displayed most potent activity EC 50...

Abstract Hit, Lead & Candidate Discovery To discover succinate dehydrogenase inhibitors with a novel structure, we introduced cinnamic acid structure to optimize the lead 1 and synthesized four series of cinnamon–pyrazole carboxamide derivatives. The bioassay data showed that compounds (E)‐N‐(1‐[4‐chlorophenyl]‐4‐cyano‐1H‐pyrazol‐5‐yl)‐3‐(2‐fluorophenyl) acrylamide ( 5III‐d) (E)‐3‐(2‐chlorophenyl)‐N‐(1‐[4‐chlorophenyl]‐4‐cyano‐1H‐pyrazol‐5‐yl) 5III‐f) significant antifungal activity...

Plant pathogenic fungi seriously threaten agricultural production. There is an urgent need to develop novel fungicides with low toxicity and high efficiency. In this study, we designed synthesized 44 pyrazolo[3,4-d]pyrimidin-4-one derivatives evaluated them for their fungicidal activities. The bioassay data revealed that most of the target compounds possessed moderate in vitro antifungal Especially compound g22 exhibited remarkable activity against Sclerotinia sclerotiorum EC50 value 1.25...

Development of novel chiral antifungal agents for effective control plant pathogens is urgently needed. In this study, a series pyrazol-5-yl-benzamide derivatives containing oxazoline moiety were rationally designed and developed based on molecular docking. The in vitro assay results indicated that compounds (rac)-4h (R1 = Et), (S)-4 h S-Et) (R)-4 R-Et) exhibited remarkable activities against Valsa mali with median concentration (EC50) values 0.24, 0.06 1.08 mg/L, respectively. Preliminary...

The utilization of novel organic synthesis methods is increasingly critical in the development innovative agrochemicals. In this study, we designed and synthesized a series chiral oxazoline derivatives using one-pot method. This method involved first catalyzing asymmetric aldol addition reaction oxazolinyl esters with paraformaldehyde, followed by esterification various pharmacophore-containing carboxylic acids. Unexpectedly, many target compounds exhibited promising antifungal antioomycete...

Abstract BACKGROUND A substantial amount of empirical research indicates that the development novel pesticides through intermediate derivatization method can significantly enhance success rate new pesticide creation while reducing and costs. In response to this demand, a series derivatives containing pyrazole imidazo[5,1‐b]thiazole were synthesized by modify imine skeleton, which was found have good antifungal activity in previous work, subjecting it intramolecular nucleophilic substitution...

A series of novel pyrazole amide derivatives 3a-3p which take TMV PC protein as the target has been designed and synthesized by reactions 5-chloro-1-aryl-3-methyl-1H-pyrazole-4-carboxylic acids with 5-amino-1-aryl-1H-pyrazole-4-carbonitriles. All compounds were characterized 1H-NMR, mass spectroscopy elemental analysis. Preliminary bioassays indicated that all acted against tobacco mosaic virus (TMV) different in vivo vitro modes at 500 μg/mL found to possess promising activity. Especially,...

To develop new antibacterial agents, a series of novel triazole-containing pyrazole ester derivatives were designed and synthesized their biological activities evaluated as potential topoisomerase II inhibitors. Compound 4d exhibited the most potent activity with Minimum inhibitory concentration (MIC) alues 4 µg/mL, 2 0.5 µg/mL against Staphylococcus aureus, Listeria monocytogenes, Escherichia coli, Salmonella gallinarum, respectively. The in vivo enzyme inhibition assay displayed (IC50 =...

Abstract BACKGROUND To promote the discovery and development of new fungicide with novel scaffolds or modes action, a series 5‐(2‐chloroethyl)‐1‐phenyl‐6‐(pyridin‐4‐yl)‐1,5‐dihydro‐4H‐pyrazolo[3,4‐d]pyrimidin‐4‐one derivatives were synthesized, evaluated for their antifungal activities. RESULTS The bioassay data showed that compound 8IIId (EC 50 = 1.93 mg L −1 ) is superior to boscalid 6.71 against Valsa mali . We introduced chiral groups on structure 8IIId, two configurations respectively...