GABA Channel Antagonist Pesticides for Resistant Weevils
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Solution Overview
Problem
Current insecticides for controlling Curculionidae family insects, such as Anthonomus, are ineffective due to resistance and pose environmental and health risks, necessitating a new class of pesticides that target the gamma-aminobutyric acid (GABA)-gated chloride channel.
Innovation Solution
Development of compounds with a partially saturated heterocycle substituted by a haloalkyl group and aromatic or heteroaromatic rings, specifically designed to antagonize the GABA-gated chloride channel, which are effective against resistant Anthonomus species in cotton crops.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Reliability
If endosulfan is used to control Curculionidae insects, then insect control effectiveness is improved, but environmental and health safety deteriorates
Solution Approach 1:
The patent changes the chemical structure parameters of insecticides by introducing compounds with partially saturated heterocycles substituted by haloalkyl groups and aromatic or heteroaromatic rings that antagonize GABA-gated chloride channels, providing effective control while improving safety profiles
Solution Approach 2:
The patent creates new chemical compounds that copy and optimize the mechanism of action of effective insecticides while eliminating harmful properties, specifically designing GABA-gated chloride channel antagonists with improved safety characteristics
2Reliability
If pyrethroids such as cyfluthrin and betacyfluthrin are used to control Curculionidae insects, then insect control effectiveness is improved, but resistance development worsens
Solution Approach 1:
The patent introduces a new chemical intermediary mechanism by designing compounds that antagonize GABA-gated chloride channels, providing an alternative pathway for insect control that bypasses resistance mechanisms developed against pyrethroids
Solution Approach 2:
The patent changes the mode of action parameters by developing compounds with partially saturated heterocycles substituted by haloalkyl groups that target GABA-gated chloride channels, creating a new mechanism that overcomes pyrethroid resistance
3Adaptability or versatility
If new compounds with partially saturated heterocycles substituted by haloalkyl groups are developed to antagonize GABA-gated chloride channel, then resistance to existing insecticides is overcome, but compound complexity increases
Solution Approach 1:
The patent segments the molecular structure into distinct functional components: a partially saturated heterocycle core substituted by haloalkyl groups and aromatic or heteroaromatic rings, allowing systematic optimization of each segment for resistance overcoming while managing overall complexity
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 provide a novel solution for controlling resistant Anthonomus weevils, effectively safeguarding cotton crops by targeting the GABA-gated chloride channel, thereby overcoming the limitations of existing insecticides.
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, preferably for controlling and/or preventing infestation of boll weevil in cotton, comprising applying to a crop of cotton plants, the locus thereof, or propagation material thereof, a compound of formula (I), wherein -B1-B2-B3 - is -C=N-O-, -C=N-CH2-, -C=CH-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 R1 is C1-C4alkyl, C1C4aloalkyl 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.