Synthesis and Antifungal Activities of New Type β-Methoxyacrylate-Based StrobUurin Analogues  

作　　者：张翔 刘慧君 高永鑫 王会利 郭宝元 李建中 

机构地区：[1]Research Center for Eco-Environmental Sciences,Chinese Academy of Sciences,Beijing 100085,China

出　　处：《Chinese Journal of Chemistry》2012年第7期1517-1524,共8页中国化学（英文版）

基　　金：Supporting information for this article is available on the WWW under http：//dx.doi.org/10.1002/cjoc.201200101 or from the author.Acknowledgement This work has been funded by the National Natural Science Foundation of China （No. 20807052） and Innovative Program of the Chinese Academy of Sciences （No. KZCX2-YW-JS403）.

摘　　要：Strobilurins have become one of the most important classes of agricultural fungicides. To discover new strobilurin derivatives with high activity against resistant pathogens, a series of novel fl-methoxyacrylate analogues were designed and synthesized by integrating substituted pyrimidine with a strobilurin pharmacophore. The compounds were confirmed and characterized by infrared, 1H nuclear magnetic resonance, elemental analysis and mass spectroscopy. The bioassays indicated that most of the compounds 1 exhibited potent antifungal activity against Colletotrichum orbiculare, Botrytis cinerea Pers and Phytophthora capsici Leonian at the concentration of 50 μg/mL. Exhilaratingly, compound 1 a （R= methyl） showed better antifungal activity against all the tested fungi than the commercial strobilurin fungicide azoxystrobin.Strobilurins have become one of the most important classes of agricultural fungicides. To discover new strobilurin derivatives with high activity against resistant pathogens, a series of novel fl-methoxyacrylate analogues were designed and synthesized by integrating substituted pyrimidine with a strobilurin pharmacophore. The compounds were confirmed and characterized by infrared, 1H nuclear magnetic resonance, elemental analysis and mass spectroscopy. The bioassays indicated that most of the compounds 1 exhibited potent antifungal activity against Colletotrichum orbiculare, Botrytis cinerea Pers and Phytophthora capsici Leonian at the concentration of 50 μg/mL. Exhilaratingly, compound 1 a （R= methyl） showed better antifungal activity against all the tested fungi than the commercial strobilurin fungicide azoxystrobin.

关 键 词：SYNTHESIS strobilurin derivatives antifungal activities substituted pyrimidine SAR 

分 类 号：TQ455.4[化学工程—农药化工] TQ463.53