文献类型：期刊文献

英文题名：Synthesis and In Vitro and In Vivo Biological Activity Evaluation and Quantitative Proteome Profiling of Oxadiazoles Bearing Flexible Heterocyclic Patterns

作者：Tao, Qing-Qing[1];Liu, Li-Wei[1];Wang, Pei-Yi[1];Long, Qing-Su[1];Zhao, Yong-Liang[1];Jin, Lin-Hong[1];Xu, Wei-Ming[1];Chen, Yang[1];Li, Zhong[2];Yang, Song[1,2]

机构：[1]Guizhou Univ, Ctr R&D Fine Chem, State Key Lab Breeding Base Green Pesticide & Agr, Key Lab Green Pesticide & Agr Bioengn,Minist Educ, Guiyang 550025, Guizhou, Peoples R China;[2]East China Univ Sci & Technol, Coll Pharm, Shanghai 200237, Peoples R China

年份：2019

卷号：67

期号：27

起止页码：7626

外文期刊名：JOURNAL OF AGRICULTURAL AND FOOD CHEMISTRY

收录：;EI(收录号：20192707148137);WOS:【SCI-EXPANDED(收录号:WOS:000475541800007)】；

基金：We acknowledge the financial support of National Natural Science Foundation of China (21877021, 21662009, 21702037, 31860516), the Research Project of Ministry of Education of China (20135201110005, 213033A), and Guizhou Provincial S&T Program ([2012]6012, LH [2017]7259, [2017]5788, [2017]222).

语种：英文

外文关键词：oxadiazoles; heterocyclic patterns; biological activity; quantitative proteomics

摘要：A novel series of simple 1,3,4-oxadiazoles that bear flexible heterocyclic patterns was prepared, and their biological activities in plant pathogenic bacteria, fungi, oomycetes, and Meloidogyne incognita in vitro and in vivo were screened to explore low-cost and versatile antimicrobial agents. Screening results showed that compounds, such as A(0), B-0, and C-4, were bioactive against Xanthomonas oryzae pv oryzae in vitro and in vivo, and such bioactivities were superior to those of commercial agents bismerthiazol and thiodiazole copper. Their antibacterial mechanisms were further investigated by quantitative proteomics and concentration-dependent scanning electron microscopy images. Antifungal results indicated that compound A(0) displayed a selective and better antifungal effect on Botrytis cinerea with inhibition rate of 96.8% at 50 mu g/mL. Nematocidal bioassays suggested that compound D-1 had good in vitro nematocidal activity toward M. incognita at 24, 48, and 72 h, with the corresponding insecticidal efficiency of 48.7%, 64.1%, and 87.2% at 40 mu g/mL. In vivo study further confirmed that compounds D-1 and F-2 showed nematocidal actions at 80 mu g/mL with a disease index of 1.5. Given these advantages, this kind of molecular frameworks could be a suitable platform for exploring highly efficient agrochemicals.