Fluxametamide: A novel isoxazoline insecticide that acts via distinctive antagonism of insect ligand-gated chloride channels

Asahi, Miho; Kobayashi, Masaki; Kagami, Takahiro; Nakahira, Kunimitsu; Furukawa, Yuki; Ozoe, Yoshihisa

doi:10.1016/j.pestbp.2018.02.002

Cited by 78 publications

(71 citation statements)

References 35 publications

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“…There is little influence on the bee-visiting insects. 63,64) Broflanilide (Vedira ™ , Tenebenal ™ , Mitsui Chemicals Agro), currently being jointly developed with BASF, has a unique chemical structure characterized as a meta-diamide and exhibits high activity against various pests, including lepidopteran, coleopteran, and thysanopteran pests. 65,66) Broflanilide received the first registration worldwide in Australia in January 2020.…”

Section: Trends In Novel Insecticides Other Than Nicotinic and Diamidementioning

confidence: 99%

Development of novel pesticides in the 21st century

2020

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General trends and strategies for novel pesticides are summarized. Global pesticide sales and pesticide discovery research are also briefly reviewed. At least 105 chemical pesticides have been launched during the past decade or are under development: 43 fungicides, 34 insecticides/acaricides, 6 nematicides, 21 herbicides, and 1 herbicide safener. Most of them are safe to humans and environmentally friendly. The most developed fungicides are SDHI (succinate dehydrogenase inhibitors), DMI (demethylation inhibitors), QoI (quinone outside inhibitors), and QiI (quinone inside inhibitors). Due to the development of resistance to fungicides with existing modes of action, many fungicides possessing various novel modes of action have been launched or are under development. The trend of insecticide development is changing from organophosphorus, carbamate, and synthetic pyrethroids to nicotinic and diamide insecticides. During the past decade, compounds possessing a variety of novel modes of action have also been launched or are under development. Flupyradifurone and flupyrimin, exhibiting extremely low honeybee toxicity, have been developed and subjected to practical use. Herbicides possessing varied modes of action, such as acetolactate synthase, p-hydroxyphenylpyruvate dioxygenase, protoporphyrinogen oxidase, and very-long-chain fatty acid elongase inhibition, have been developed, but no herbicides possessing a novel mode action have commercialized in nearly 30 years. It is of interest that cyclopyrimorate, which was recently launched, and tetflupyrolimet, which is under development, have novel modes action: homogentisate solanesyltransferase (HST) and dihydroorotate dehydrogenase (DHODH) inhibition, respectively. The development of useful acaricides and nematicides is also progressing. Some natural product origin pesticides are getting attention.

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Section: Trends In Novel Insecticides Other Than Nicotinic and Diamidementioning

confidence: 99%

Development of novel pesticides in the 21st century

2020

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“…Fluxametamid (Fig. 4), is a racemic isoxazoline insecticide (contains an isomeric methoxime group) that demonstrates high activity against various lepidopteran, thysanopteran and dipteran pest species 20 . It is also acaricidal active against tetranychid mites (Acari: Tetranychidae ).…”

Section: Novel Mechanisms Of Actionmentioning

confidence: 99%

Status and outlook for acaricide and insecticide discovery

Jeschke

2020

Pest Management Science

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To guarantee sustainability and progress, the agrochemical industry is faced with several major challenges. Currently, loss of active ingredients due to consumer perception, changing grower needs and ever-changing regulatory requirements is far higher than the number being introduced into the market. Therefore, there is a need to develop new products that can provide improved efficacy, selectivity and favorable environmental profiles. Strategies to achieve these goals are the search for acaricides and insecticides with new modes of action, or the discovery of novel molecules with activity on the most attractive target sites having resistance breaking properties against pest species. In this context, the introduction of halogen atoms or asymmetric centers into an active ingredient remains an important tool to modulate their properties, but so too is the pro-pesticide concept. This review gives an overview of agrochemicals launched over the past 8 years, reflects new insights into known mechanisms of action, and describes the status and outlook for acaricide and insecticide discovery. Supporting information may be found in the online version of this article.

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“…In insects, γ-aminobutyric acid receptors (GABARs) are the major inhibitory receptors widely distributed in the central nervous system 19 and are the target of natural compounds (picrotoxin) and synthetic pesticides (such as dieldrin, fipronil, fluxametamide and fluralaner) 20-22 . According to the classification of the Insecticide Resistance Action Committee (https://irac-online.org/modes-of-action/, IRAC), Compounds that act on GABAR are divided into two categories: blockers (Category 2, represented by fipronil and chlordane) and allosteric modulators (Category 30, represented by broflanilide and fluxametamide) (referred to as GABAR compounds in this paper).…”

Section: Introductionmentioning

confidence: 99%

BacterialPxRdl2dsRNA increased the insecticidal activities of GABAR-targeting compounds againstPlutella xylostella

Wang

et al. 2021

Preprint

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BACKGROUND: The application of RNAi to control pests has attracted the attention of researchers. Our results indicated that knockout of PxRdl2 can decrease resistance to fipronil in Plutella xylostella, providing a suitable target gene for RNAi-based pest control. RESULTS: The differences in the sensitivity of two established homozygous knockout strains of P. xylostella. (Rdl1KO and Rdl2KO) and susceptible P. xylostella to a series of compounds were evaluated. Quinazolines and isoxazolines both showed stronger efficacy in the Rdl2KO strain. Therefore, we proposed a method based on the knockdown of the P. xylostella Rdl2 gene as a tactic to enhance the toxicity of quinazolines and isoxazolines. To reduce costs and protect dsRNA against degradation, we applied a bacterial expression system using the L4440 vector to express PxRdl2 dsRNA in HT115 Escherichia coli. Transformed bacteria (dsRNA-Bac) fed through leaves combined with quinazoline and isoxazolines proved to be more effective in both the susceptible and fipronil-resistant P. xylostella. CONCLUSION: Our results provide a strategy for the development of novel insecticide spray formulations containing dsRNA-Bac, which synergize with insecticide toxins by suppressing PxRdl2, reducing the use of pesticides in the field.

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Fluxametamide: A novel isoxazoline insecticide that acts via distinctive antagonism of insect ligand-gated chloride channels

Cited by 78 publications

References 35 publications

Development of novel pesticides in the 21st century

Development of novel pesticides in the 21st century

Status and outlook for acaricide and insecticide discovery

BacterialPxRdl2dsRNA increased the insecticidal activities of GABAR-targeting compounds againstPlutella xylostella

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