Chinese Journal of Organic Chemistry >
Design, Synthesis and Biological Activities of N-(Substitutedbenzoyl)-N'-(5-methoxyl-2-methylsulfanylpyrimidin-4-amino)(thio) Ureas
Received date: 2014-04-24
Revised date: 2014-05-20
Online published: 2014-07-02
Supported by
Project supported by the Promotive Research Fund for Excellent Young and Middle-aged Scientists of Shandong Province (No.BS2011NY013), the Innovation Fund for the Youth of Shandong Agricultural University (No.23682), the National Natural Science Foundation of China (No.21102173), the Project of Development of Science and Technology of Shandong Province (No.2013GZX20109) and the President Science Foundation of South China Agricultural University (No.4200-K13014).
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, α-methoxyl methyl acetate and ethyl formate. Their structures were confirmed by 1H 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 mg/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 2~3 instar Culex larvae, compounds 10o and 10r showed 97.8% revised uneclosion rate, and compound 10t exhibited 100% insecticidal activity.
Li Chengkun , Jiang Lin , Wang Yue , Wan Fuxian , Zhang Peizhi , Li Ying , Cui Zining . Design, Synthesis and Biological Activities of N-(Substitutedbenzoyl)-N'-(5-methoxyl-2-methylsulfanylpyrimidin-4-amino)(thio) Ureas[J]. Chinese Journal of Organic Chemistry, 2014 , 34(11) : 2296 -2303 . DOI: 10.6023/cjoc201404043
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