Azoline Compounds for Broad-Spectrum Insecticidal Control
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Solution Overview
Problem
Current pesticidal agents against invertebrate pests, particularly arthropods and nematodes, face issues with resistance development and persistence in the environment, leading to economic losses and the need for new compounds with broader activity spectra and reduced toxicity.
Innovation Solution
Development of azoline compounds with specific stereoisomers and salts that exhibit potent insecticidal activity against a wide range of invertebrate pests, including difficult-to-control arthropods and nematodes, while being less persistent and bioaccumulative than existing isoxazoline insecticides.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Reliability
If isoxazoline insecticides are used to control invertebrate pests, then pesticidal activity is improved, but environmental persistence and bioaccumulation increase
Solution Approach 1:
The patent modifies the chemical structure of isoxazoline compounds by changing specific parameters: replacing the isoxazoline ring with azoline variants (isoxazolidine, dihydroisoxazole, isoxazole), modifying substituent groups at positions R1, R2, R3, R4, and R5, and adjusting molecular weight and lipophilicity parameters. These parameter changes reduce environmental persistence while preserving pesticidal activity against invertebrate pests.
2Reliability
If existing pesticidal agents are used repeatedly, then pest control effectiveness is improved, but resistance development in target pests increases
Solution Approach 1:
The patent introduces novel chemical structures with modified molecular parameters compared to existing isoxazoline insecticides. By changing the core ring structure from isoxazoline to various azoline configurations and modifying substituent patterns, the compounds present new molecular targets that pest populations have not developed resistance against, thereby maintaining control effectiveness while overcoming resistance issues.
3Reliability
If high potency insecticides are used to control difficult-to-control arthropods, then pest elimination is improved, but toxicity to the environment increases
Solution Approach 1:
The patent applies local quality modification by introducing specific substituent groups at particular positions on the molecular structure. For example, adding electron-withdrawing groups at R2 or R4 positions, or introducing specific alkyl and aryl substituents at R1 and R5, creates localized electronic and steric effects that enhance binding affinity to pest targets while reducing non-specific toxicity to environmental organisms.
Solution Approach 2:
The patent optimizes the balance between potency and toxicity by adjusting molecular parameters such as logP (lipophilicity), molecular weight, and hydrogen bond donors/acceptors. The modified azoline compounds are designed with parameters that favor selective toxicity toward invertebrate pests while minimizing harm to mammals and the environment, achieving high elimination efficacy with reduced environmental toxicity.
Data Source
AI summary
The present invention relates to azoline compounds of formula (I) wherein A, B1, B2, B3, G1, G2, X1, R1, R3a, R3b, Rg1 and Rg2 are as defined in the claims and the description. The compounds are useful for combating or controlling invertebrate pests, in particular arthropod pests and nematodes. The invention also relates to a method for controlling invertebrate pests by using these compounds and to plant propagation material and to an agricultural and a veterinary composition comprising said compounds.