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SYP-34773 is a pyrimidinamine derivative and a novel fungicide modified from diflumetorim. This study determined the antimicrobial spectrum of SYP-34773, which showed it could strongly inhibit the growth of some important plant pathogens including fungi and oomycetes. In particular, Phytophthora infestans is an oomycete sensitive to SYP-34773, and the mycelium growth stage was found to be the most sensitive stage, with an EC50 value of 0.2030 μg/mL. At a concentration of 200 μg/mL, SYP-34773 displayed an excellent control efficacy of 69.55% and 81.48% against potato and tomato blight disease caused by P. infestans under field conditions, respectively. Mode of action investigations showed that this fungicide could cause severe ultrastructure damage to the mycelia of P. infestans, inhibit its respiration, and increase the cell membrane permeability of this pathogen. The results of this study could provide useful information for the fungicide registration and application of SYP-34773 as a novel fungicide.

Laccase is a potential target for novel agricultural fungicide discovery.

On the basis of the structure of nicotlactone A (

To develop novel succinate dehydrogenase inhibitors (SDHIs), two series of novel

Fluoxapiprolin is a new piperidinyl thiazole isoxazoline fungicide developed by Bayer Crop Science in 2012, but the sensitivity and resistance mechanism of fluoxapiprolin are unclear. In this study...

As a continuous effort toward developing novel and highly efficient agrochemicals for integrated management of crop pathogens, two series of oxime ester derivatives from indole and tetrahydroquinoline natural scaffolds were prepared. Guided by the preliminary inhibition rates against ubiquitous and representative fungi, the antifungal profile of the target compounds against

R034-1 is a new member of the piperidinyl thiazole isoxazoline class of fungicides that shows high activity against most plant-pathogenic oomycetes and could effectively inhibit several developmental stages of Phytophthora capsici. Here, the potential resistance risk for R034-1 was evaluated in P. capsici. The baseline sensitivities of 135 isolates to R034-1 showed a unimodal curve, with a mean EC50 value of 0.004 μg/mL. Twelve resistant mutants were generated by fungicide adaptation and displayed lower fitness compared to parental isolates, which suggests that the resistance risk of P. capsici to R034-1 is low. R034-1 and oxathiapiprolin are structurally related, and resistant isolates display cross-resistance to both compounds, suggesting that these fungicides may target the same oxysterol binding protein. Comparison of PcORP1 genes in the resistant mutants and their parental isolates revealed (N767S, N767I, and G700V) amino acid substitutions in the R034-1 resistant mutant. Causality was functionally validated using site-directed mutagenesis of the target gene using the CRISPR/Cas9 system.

Our aim was to investigate the bioactivity and mode of action of a novel fungicide 4-chlorocinnamaldehyde thiosemicarbazide (PMDD). As a result of its efficacy against various plant pathogens, its protective fungicidal activity, and systemic transport after root treatment, PMDD could be a promising fungicide to control wheat root diseases. In a field assay, PMDD showed good control efficacy on wheat take-all disease. A biochemical study indicated that PMDD acts as a laccase inhibitor, a to date unique mode of fungicidal action. Moreover, a total of seven stable PMDD-resistant Gaeumannomyces graminis var. tritici (Ggt) mutants were generated and demonstrated no cross-resistance with any commercial fungicides used for take-all disease control, and the gene expression profile further confirmed that laccase could be the target of PMDD. Taken together, we conclude that PMDD is a laccase inhibitor and could be used on wheat to control take-all diseases. The current study could strongly benefit the registration and application of PMDD.

Laccase is a novel target for fungicides. We previously developed a new fungicide, 4-chlorocinnamaldehyde thiosemicarbazide (PMDD-5Y), as a laccase inhibitor. The introduction of active groups of natural products into the framework of a pesticide molecular structure is an effective method for discovering active lead compounds, and it has applications in the discovery of new pesticides. In this work, PMDD-5Y was selected as a lead compound, and we designed and synthesized a series of novel sulfonyl hydrazide derivatives containing the natural product scaffold 1,2,3,4-tetrahydroquinoline. The new compounds had antifungal activities against several fungi, especially

SYP-34773 is a pyrimidinamine derivative and a novel fungicide modified from diflumetorim. This study determined the antimicrobial spectrum of SYP-34773, which showed it could strongly inhibit the growth of some important plant pathogens including fungi and oomycetes. In particular

Fluoxapiprolin is a new piperidinyl thiazole isoxazoline fungicide developed by Bayer Crop Science in 2012, but the sensitivity and resistance mechanism of fluoxapiprolin are unclear. In this study, the sensitivities of 130

R034-1 is a new member of the piperidinyl thiazole isoxazoline class of fungicides that shows high activity against most plant-pathogenic oomycetes and could effectively inhibit several developmental stages of

Our aim was to investigate the bioactivity and mode of action of a novel fungicide 4-chlorocinnamaldehyde thiosemicarbazide (PMDD). As a result of its efficacy against various plant pathogens, its protective fungicidal activity, and systemic transport after root treatment, PMDD could be a promising fungicide to control wheat root diseases. In a field assay, PMDD showed good control efficacy on wheat take-all disease. A biochemical study indicated that PMDD acts as a laccase inhibitor, a to date unique mode of fungicidal action. Moreover, a total of seven stable PMDD-resistant

Previous research has demonstrated that 3-[5-(4-chlorophenyl)-2,3-dimethyl-3-isoxazolidinyl]pyridine (SYP-Z048), a newly developed nitrogen heterocycle substituted isoxazolidine compound, has good protective and curative activities against a wide range of fungal diseases of fruits and vegetables caused by Ascomycetes, Basidiomycetes, and Deuteromycetes. In this study, the photochemical behavior of SYP-Z048 was investigated in aqueous solution and in response to solar and low-pressure mercury ultraviolet (UV) lamp irradiation. SYP-Z048 photolysis was pH- and temperature-dependent and was described by a first-order degradation reaction. A total of 11 photoproducts were separated by high-performance liquid chromatography (HPLC) and solid-phase extraction (SPE) and were identified on the basis of (1)H and (13)C nuclear magnetic resonance (NMR) and high-performance liquid chromatography-mass spectrometry (HPLC-MS) spectra. The photoproduct structures and kinetics suggested that the phototransformation of SYP-Z048 occurred via multiple reaction pathways that included the cleavage of the N-O bond in the isoxazolidine ring and the dechlorination of the benzene ring.