【作者】 王志鹏； 李建强； 高扬； 于淑晶； 寇俊杰； 王红学； 赵卫光；

【Author】 WANG Zhi-peng;LI Jian-qiang;GAO Yang;YU Shu-jing;KOU Jun-jie;WANG Hong-xue;ZHAO Wei-guang;State Key Laboratory of Elemento-Organic Chemistry,Nankai University;

【机构】 南开大学元素有机化学国家重点实验室；

【摘要】 [目的]纤维素合成酶是缬氨酸酰胺类杀菌剂的作用靶标。氨基酸类杀菌剂由于其良好的环境相容性和低毒性,成为农药研究中的重要研究方向。[方法]以商品药剂异丙菌胺为先导,在苯环和氨基之间引入了OCH₂链,设计合成了一系列新的缬氨酸酰胺类杀菌剂,并研究了其杀菌活性和构效关系。[结果]结果表明,目标化合物具有良好的杀菌剂活性,其中苯环对位炔丙氧基取代的化合物的对辣椒疫霉的杀菌活性与异丙菌胺相当,并且对非卵菌纲病害也有较好的杀菌活性。[结论]新型缬氨酸酰胺类杀菌剂具有进一步开发成商品药的前景。更多还原

【Abstract】 [Aims]Cellulose synthases are a significant action targets for carboxylic acid amide fungicides.The valinamide carbamates,as amino acids fungicides,undoubtedly are an excellent alternative to synthetic pesticides as a means to reduce negative impacts to human health and the environment.[Methods]As a continuation of research work on the development of new cellulose synthases inhibitors,a series of the "stretched" analogues of iprovalicarb,an important commercial fungicide,were designed and synthesized by the introduction of an additional OCH₂ linker.[Results]The bioassay results indicated that the series 7 containing small group atp-position of phenyl have excellent fungicidal activities with EC50 values ranging from 0.23 to5.64 μg mL^-1.Most interestingly,propgyloxy group led to a significant increase in fungicidal activity,compounds 7o with propgyloxy group was identified as the most promising candidate due to its excellent fungicidal potency against oomycete diseases and good fungicidal activity against non-oomycete diseases.[Conclusions]This work demonstrates that a few compounds possessed excellent activities against oomycete diseases and good activities against non-oomycete diseases,among which 7o behaved the best and can be used as potential antigungidal agent.更多还原