GABA Antagonist Pesticides for Wireworm Control
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Solution Overview
Problem
Current methods for controlling wireworms are ineffective, especially against resistant strains, and there is a need for a new class of pesticides that can target wireworms in a more effective manner.
Innovation Solution
The use of compounds that are gamma-aminobutyric acid (GABA)-gated chloride channel antagonists with a partially saturated heterocycle substituted by a haloalkyl substituent and one or two aromatic or heteroaromatic rings, applied to the locus of useful plants, such as corn, to control and prevent wireworm infestations.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Reliability
If current insecticides are used to control wireworms, then wireworm control is achieved, but resistant strains develop making the control ineffective
Solution Approach 1:
The patent applies parameter changes by introducing a novel chemical structure class (formula I compounds with specific heterocyclic cores, aromatic rings, and haloalkyl substituents) that acts on a different physiological target (GABA-gated chloride channels) compared to conventional insecticides. This fundamental parameter change in the active ingredient's molecular structure and mode of action effectively controls wireworms while preventing resistance development to existing insecticide classes
2Reliability
If new compounds are developed to target resistant wireworms, then control effectiveness improves, but the complexity of the pesticide class increases
Solution Approach 1:
The patent applies local quality by identifying and emphasizing specific structural features within the complex molecule that are critical for activity against wireworms. The heterocyclic core (partially saturated 5- or 6-membered ring), aromatic or heteroaromatic rings, and haloalkyl substituents are positioned and configured to interact with specific binding sites on GABA-gated chloride channels, providing targeted effectiveness while managing complexity through focused structural design
Applied Scientific Principles
This section explains which scientific principles are used to turn an abstract innovation direction into a practical engineering solution.
Function Achieved in This Case
These compounds demonstrate high efficacy in controlling wireworms, including resistant strains, through direct soil application, in-furrow application, or seed treatment, providing effective prevention and reduction in wireworm damage to crops.
Implementation Method 1
Compounds that are insecticidally, acaricidally, nematicidally and/or moluscicidally active by antagnonism of the gamma-aminobutyric acid (GABA)-gated chloride channel
Data Source
AI summary
The present invention relates to methods of controlling and/or preventing soil-dwelling pests in useful plants comprising applying to the locus of the useful plant or treating plant propagation material thereof with a compound of formula (I) wherein -B1-B2-B3- is -C=N-O-, -C=N-CH2-, -C=CH2-O- or -N-CH2-CH2-; L is a direct bond or methylene; A1 and A2 are C-H, or one of A1 and A2 is C-H and the other is N; X1 is group X, formula (X) R1 is C1-C4alkyl, C1-C4aloalkyl or C3-C6cycloalkyl; R2 is chlorodifluoromethyl or trifluoromethyl; each R3 is independently bromo, chloro, fluoro or trifluoromethyl; R4 is hydrogen, halogen, methyl, halomethyl or cyano; R5 is hydrogen; or R4 and R5 together form a bridging 1,3-butadiene group; p is 2 or 3. Preferably the soil-dwelling pest is selected from corn rootworm, wireworms, grubs, in particular white grubs (e.g. Phyllophaga sp., Diloboderus sp., Popillia japonica), termites (in particular for sugar cane), subterraneous stinkbugs (e.g. Scaptocoris sp.), cutworms (e.g. agrotis sp.), millipedes (e.g. Julus sp.) and broca gigante (e.g. Telchin licus).