Pest Management Science · 2010 · 37 citations · 8 references
PharmacyChemistryMedicinal ChemistryBioisosterismDrug DiscoveryStructure-activity RelationshipsBioisosteric DesignBioisosteric ReplacementLead Compound DesignLead DiscoveryNatural Product Drug DiscoveryPotency OptimizationActive Compound IsolationChemical Synthesis Of AnaloguesLead Compound IdentificationPyrimidine AnalogsPyrimidine AnaloguesPyrimidine BioisosteresToxicity BioassaysX-ray Diffraction Analysis
BACKGROUND: The intermediate derivatisation method based on bioisosteric replacement led to the discovery of the lead strobilurin compound 5a. To produce new strobilurin analogues with improved activity, a series of substituted pyrimidines were synthesised and bioassayed. RESULTS: The compounds were identified by (1)H NMR, IR, MS and elemental analysis. The highly active compound 5 g was studied by X-ray diffraction. Preliminary bioassays demonstrated that some of the title compounds exhibited excellent acaricidal activity against Tetranychus cinnabarinus (Boisd.) at 10 mg L(-1). The relationship between structure and acaricidal activity is reported. CONCLUSION: The present work demonstrates that strobilurin derivatives containing pyrimidine moieties can be used as possible lead compounds for developing novel acaricides.
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Review: Approaches to New Parasiticides
Michael Londershausen · Pesticide Science · 1996 · 141 citations