Design, Synthesis and Biological Activities of N-(Substituted benzoy1)-N′-(5-methoxyl-2-methylsulfanylpyrimidin-4-amino)(thio) Ureas

In order to find new lead compounds with high effciency, low toxicity and environmental-friendly contribution, a series of novel N-(substituted benzoyl)-N'-(5-methoxyl-2-methylsulfanylpyrimidin-4-amino)(thio) ureas were designed and synthesized from substituted benzoic acids, alpha-methoxyl methyl acetate and ethyl formate. Their structures were confirmed by H-1 NMR, IR and elemental analysis. The preliminary bioassay results indicated that some compounds exhibited considerate fungicidal activity. Among them compounds 10m and 10p showed more than 70% inhibitory rate to Botrytis cinerea and Sclerotinia sclerotiorum at 50 mu g/mL, and the inhibitory rate against Sclerotinia sclerotiorum was higher than the control fungicide 95% chlorothalonil. Some compounds showed obvious insect growth regulation activity against 2 similar to 3 instar Culex larvae, compounds 10o and 10r showed 97.8% revised uneclosion rate, and compound 10t exhibited 100% insecticidal activity.