Abstract
In order to find pesticides with insecticidal and antifungal activities, a series of novel benzoyl pyrimidinylurea derivatives were designed and synthesized. All target compounds were identified by 1H-NMR spectroscopy and HRMS. Insecticidal and antifungal activity of these compounds were evaluated and the structure-activity relationships (SAR) were clearly and comprehensively illustrated. Compound 7, with low toxicity to zebrafish (LC50 = 378.387 µg mL−1) showed 100% inhibition against mosquito (Culex pipiens pallens) at 0.25 µg mL−1. Both compounds 19 and 25 exhibited broad-spectrum fungicidal activity (>50% inhibitory activities against 13 phytopathogenic fungi), which were better than those of the commercial pesticide pyrimethanil (>50% inhibitory activities against eight phytopathogenic fungi). Furthermore, compounds 19 and 25 exhibited protective activity against Sclerotinia sclerotiorum on leaves of Brassica oleracea L. during in vivo experiments.
Highlights
Plant disease and pest control are at least as old as agriculture because there is a need to keep crops free of pests and phythopatogenic fungi
In order structure-activity relationship of compounds, the order to to comprehensively comprehensivelyanalyze analyzethethe structure-activity relationship of compounds, chemical structures of the benzoylpyrimidinylureas was separated into three units, namely, the the chemical structures of the benzoylpyrimidinylureas was separated into three units, namely, benzoyl ring (A), ring (B) and
Ia–p were synthesized used asfor starting materials synthesis of the (Schemes and target compounds (Schemes 1 and 2)
Summary
Plant disease and pest control are at least as old as agriculture because there is a need to keep crops free of pests and phythopatogenic fungi. Dimilin (diflubenzuron) (Figure 1), introduced in the market at 1975, exhibits broad spectrum larvicidal activities against caterpillars (Pieris brassicae), mosquitoes (Aedes aegypti), houseflies (Musca domestica), desert locust (Schistocera gregaria) and cotton strainers (Dysdercus superstitiosus) [3]. In the past few years, we and our co-workers have designed and synthesized several series of benzoylphenylureas (A and B, Figure 1) and most compounds exhibited excellent insecticidal activities against oriental armyworm (Mythimna separata) or mosquito (Culex pipiens pallens) [4,5,6,7,8]. Compounds C and D (Figure 1) with a 2,2,2-trifluoroethyl group (R = CH2 CF3 ) substituent, displayed much better insecticidal activities against oriental armyworm than other derivatives.
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