文献类型：期刊文献

英文题名：Synthesis of Thiazolium-Labeled 1,3,4-Oxadiazole Thioethers as Prospective Antimicrobials: In Vitro and in Vivo Bioactivity and Mechanism of Action

作者：Wang, Ming-Wei[1];Zhu, Huai-He[1];Wang, Pei-Yi[1];Zeng, Dan[1];Wu, Yuan-Yuan[1];Liu, Li-Wei[1];Wu, Zhi-Bing[1];Li, Zhong[2];Yang, Song[1,2]

机构：[1]Guizhou Univ, State Key Lab Breeding Base Green Pesticide & Agr, Key Lab Green Pesticide & Agr Bioengn, Ctr R&D Fine Chem,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：46

起止页码：12696

外文期刊名：JOURNAL OF AGRICULTURAL AND FOOD CHEMISTRY

收录：;EI(收录号：20194607697055);WOS:【SCI-EXPANDED(收录号:WOS:000499743400011)】；

基金：The authors are grateful for the funds from China's NSFC (21877021, 21702037, 31860516, 21662009); R.P. Ministry of Education (20135201110005, 213033A); and Guizhou PS&TP (LH [2017]7259, [2012]6012, [2017]5788).

语种：英文

外文关键词：1,3,4-oxadiazole; thiazolium; antimicrobial; 3D-QSAR; proteomics; action mechanism

摘要：In this study, a type of thiazolium-labeled 1,3,4-oxadiazole thioether bridged by diverse alkyl chain lengths was constructed. The antimicrobial activity of the fabricated thioether toward plant pathogenic bacteria and fungi was then screened. Antibacterial evaluation indicated that title compounds possess specific characteristics that enable them to severely attack three phytopathogens, namely, Xanthomonas oryzae pv. oryzae, Ralstonia solanacearum, and Xanthomonas axonopodis pv. citri with minimal EC50 values of 0.10, 3.27, and 3.50 mu g/mL, respectively. Three-dimensional quantitative structure-activity relationship models were established to direct the following excogitation for exploring higher active drugs. The in vivo study against plant bacterial diseases further identified the prospective application of title compounds as alternative antibacterial agents. The proteomic technique, scanning electron microscopy patterns, and fluorescence spectrometry were exploited to investigate the antibacterial mechanism. Additionally, some target compounds performed superior inhibitory actions against three tested fungal strains. In view of their simple molecular architecture and highly efficient bioactivity, these substrates could be further explored as promising surrogates for fighting against plant microbial infections.