F129L-Resistant Soybean Rust Control With Cytochrome b Compounds
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Solution Overview
Problem
The emergence of soybean rust fungi with resistance to QoI fungicides due to a specific amino acid substitution (F129L) in the cytochrome b gene reduces the efficacy of conventional fungicides like pyribencarb, azoxystrobin, dimoxystrobin, metominostrobin, and fluoxastrobin.
Innovation Solution
Application of a compound represented by formula (I) or its N oxide or agriculturally acceptable salt, which targets the mitochondrial cytochrome b protein with an amino acid substitution of F129L, effectively controlling soybean rust fungus.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Reliability
If QoI fungicides are used to control soybean rust fungus, then the fungus can be controlled effectively, but the fungus develops resistance through amino acid substitution (F129L) in cytochrome b protein
Solution Approach 1:
The patent modifies the chemical structure of QoI fungicides by changing parameters at specific positions (R1, R2, R3, R4, R5, R6, R7, R8, R9, R10, R11, R12, R13, R14, R15, R16) to create compounds with reduced affinity for the resistant F129L mutant while maintaining efficacy against wild-type fungi. This structural parameter change allows the fungicide to overcome resistance without losing effectiveness.
Solution Approach 2:
The patent divides the fungicide molecule into distinct structural segments (different R groups at various positions) that can be independently optimized. By segmenting the molecular structure, the invention can target specific interaction sites with the cytochrome b protein to bypass the F129L resistance mechanism while maintaining overall fungicidal activity.
2Ease of operation
If conventional QoI fungicides are used against resistant strains, then the treatment is simple, but the efficacy is reduced to practical problem levels
Solution Approach 1:
The patent systematically modifies molecular parameters (substituents at R1-R16 positions) to optimize the balance between binding affinity to the target enzyme and selective pressure to prevent resistance. These parameter changes result in compounds that maintain high efficacy against F129L resistant strains while preserving ease of agricultural application.
3Object-affected harmful factors
If the fungicide binds to cytochrome bc1 complex oxidation center, then respiration is suppressed and fungi are killed, but resistance develops through gene mutation
Solution Approach 1:
The patent changes the chemical parameters of the fungicide molecule to alter its binding characteristics with the cytochrome bc1 complex. The modified compounds exhibit different binding affinities and interaction mechanisms that bypass the F129L mutation effect, maintaining respiration suppression capability while overcoming the resistance mechanism.
Solution Approach 2:
The patent introduces structural intermediaries (modified R groups) that act as mediators between the fungicide and the cytochrome b protein. These intermediary structures enable the fungicide to interact with the target enzyme in a way that is not blocked by the F129L substitution, thereby maintaining effectiveness against resistant strains.
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
The compound effectively controls soybean rust fungus with the F129L substitution, restoring the efficacy of fungicides against resistant strains.
Implementation Method 1
QoI fungicides usually bind to the ubihydroquinone oxidation centers of cytochrome bc1 complex (electron transfer complex III) in mitochondria, and suppress a respiration of the phytopathogenic fungi
Data Source
AI summary
The present invention provides a method for controlling a soybean rust fungus having an amino acid substitution of F129L on mitochondrial cytochrome b protein. According to the present invention, a compound represented by formula (I) [wherein R1 represents a C1-C3 chain hydrocarbon group and so on, n is 0, 1, 2 or 3, and when is 2 or 3, a plural of R2 may be identical to or different from each other, and R2 represents a C1-C3 chain hydrocarbon group and so on, Q represents a group represented by Q1 (where • represents a binding site to a benzene ring) and so on, L1 represents CH2 or an oxygen atom, and E represents a C1-C6 alkyl group and so on.] can use to control a soybean rust fungus having an amino acid substitution of F129L on mitochondrial cytochrome b protein.