Diaryl Pyrazole Compounds for Resistant Pest Control
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Solution Overview
Problem
Current agrochemicals face challenges in providing effective insecticidal and acaricidal activity while minimizing chemical resistance, phytotoxicity, soil contamination, and toxicity to livestock and fish, and are often insufficient against resistant pest strains.
Innovation Solution
Development of diaryl pyrazole compounds with specific structural representations that serve as active ingredients in formulations for controlling harmful organisms, including ectoparasites and endoparasites, offering superior insecticidal and acaricidal activity with reduced toxicity and resistance issues.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Reliability
If conventional agrochemicals are used to control harmful organisms, then insecticidal and acaricidal activity is achieved, but chemical resistance develops and toxicity to non-target organisms increases
Solution Approach 1:
The patent modifies the chemical structure of pyrazole compounds by changing parameters such as substituting hydrogen atoms at specific positions (R1, R2, R4, R5) with various functional groups (halogeno, cyano, amino, carboxyl, etc.) and adjusting the aryl group substitutions. These structural parameter changes result in compounds with superior insecticidal and acaricidal activity while reduced toxicity to non-target organisms and lowered chemical resistance development.
Solution Approach 2:
The patent creates composite molecular structures by combining pyrazole core compounds with various aryl groups and functional substituents. This composite approach generates a diverse family of compounds (Formula I) that exhibit enhanced biological activity and improved safety profiles compared to single-structure conventional agrochemicals.
2Reliability
If existing pyrazole compounds are synthesized, then insecticidal activity is obtained, but the synthesis process is complex and costly
Solution Approach 1:
The patent divides the synthesis process into modular steps, allowing independent variation of different parts of the molecule (R1-R5 substituents and aryl groups). This segmentation enables the use of commercially available starting materials and standardized synthesis protocols, reducing overall manufacturing complexity and cost while maintaining the ability to generate diverse active compounds.
Solution Approach 2:
The patent develops a universal synthesis approach that can produce multiple compounds of Formula I from common starting materials through systematic substitution. This multi-functional synthesis strategy allows a single synthetic pathway to generate numerous variants with different activities and properties, eliminating the need for separate synthesis routes for each compound.
3Reliability
If higher concentrations of agrochemicals are used to control resistant pest strains, then efficacy is improved, but phytotoxicity and environmental contamination increase
Solution Approach 1:
The patent optimizes the concentration parameter by developing compounds with higher intrinsic activity that effective at lower concentrations. The structural modifications (substituents at R1-R5 and aryl groups) enhance binding affinity and biological activity, allowing control of resistant pest strains at reduced dosages that minimize phytotoxicity and environmental contamination.
Solution Approach 2:
The patent creates a family of compounds that are structural variants of the pyrazole core, where each variant is optimized for specific pest control applications. This copying approach allows selection of the most effective compound at the lowest effective concentration, avoiding the need to use high concentrations that cause harmful effects.
Data Source
AI summary
A compound represented by the following Formula (I) or a salt thereof, as well as a formulation for controlling harmful organisms, and in particular, an insecticidal formulation, a miticidal formulation, a formulation for controlling ectoparasites or a formulation for controlling or killing endoparasites, which contains at least one compound selected from the compounds of Formula (I) and salts thereof as an active ingredientwherein, each of R1 and R2 independently represents a hydrogen atom, a substituted or unsubstituted C1-6 alkyl group, or the like, with the proviso that when R2 represents a hydrogen atom, R1 represents a substituted or unsubstituted C6-10 aryl group or a substituted or unsubstituted 3- to 6-membered heterocyclyl group; R3 represents a C1-6 alkylthio group or the like; each of R4 and R5 independently represents a hydrogen atom, a halogeno group or the like; and Ar represents a substituted or unsubstituted C6-10 aryl group, or a substituted or unsubstituted 5- to 6-membered heteroaryl group.