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Novel BenzothiazolenDerivatives as Potential Anti-QuorumnSensing Agents for Managing Plant Bacterial Diseases: Synthesis, AntibacterialnActivity Assessment, and SAR Study 新型苯并噻唑衍生物作为植物细菌性病害潜在的抗群体感应剂：合成、抗菌活性评估和SAR研究

Figshare Pub Date : 2023-04-19 DOI: 10.1021/acs.jafc.2c07810.s001

Pan-Long Chu (12908213), Yu-Mei Feng (333805), Zhou-Qing Long (8103521), Wan-Lin Xiao (12556560), Jin Ji (2420101), Xiang Zhou (164107), Pu-Ying Qi (8476077), Tai-Hong Zhang (8805695), Heng Zhang (320479), Li-Wei Liu (1415464), Song Yang (162335)

{"title":"Novel BenzothiazolenDerivatives as Potential Anti-QuorumnSensing Agents for Managing Plant Bacterial Diseases: Synthesis, AntibacterialnActivity Assessment, and SAR Study","authors":"Pan-Long Chu (12908213), Yu-Mei Feng (333805), Zhou-Qing Long (8103521), Wan-Lin Xiao (12556560), Jin Ji (2420101), Xiang Zhou (164107), Pu-Ying Qi (8476077), Tai-Hong Zhang (8805695), Heng Zhang (320479), Li-Wei Liu (1415464), Song Yang (162335)","doi":"10.1021/acs.jafc.2c07810.s001","DOIUrl":"https://doi.org/10.1021/acs.jafc.2c07810.s001","url":null,"abstract":"As quorum sensing (QS) regulates bacterial pathogenicity,nantiquorumnsensing agents have powerful application potential for controllingnbacterial infections and overcoming pesticide/drug resistance. Identifyingnanti-QS agents thus represents a promising approach in agrochemicalndevelopment. In this study, the anti-QS potency of 53 newly preparednbenzothiazole derivatives containing an isopropanolamine moiety wasnanalyzed, and structure–activity relationships were examined.nCompound D3 exhibited the strongestnantibacterial activity, with an in vitro EC50 of 1.54 μg mL–1 against Xanthomonasnoryzae pv oryzae (Xoo).nCompound D3 suppressed QS-regulatednvirulence factors (e.g., biofilm, extracellular polysaccharides, extracellularnenzymes, and flagella) to inhibit bacterial infection. Innvivo anti-Xoo assays indicated good controlnefficiency (curative activity, 47.8%; protective activity, 48.7%)nat 200 μg mL–1. Greater control efficiencynwas achieved with addition of 0.1% organic silicone or orange peelnessential oil. The remarkable anti-QS potency of these benzothiazolenderivatives could facilitate further novel bactericidal compound development.","PeriodicalId":522264,"journal":{"name":"Figshare","volume":"1 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2023-04-19","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"147894329","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

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