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新型苯并噻唑衍生物作为管理植物细菌病害的潜在群体感应抑制剂:合成、抗菌活性评估及构效关系研究。

Novel Benzothiazole Derivatives as Potential Anti-Quorum Sensing Agents for Managing Plant Bacterial Diseases: Synthesis, Antibacterial Activity Assessment, and SAR Study.

机构信息

National Key Laboratory of Green Pesticide, Key Laboratory of Green Pesticide and Agricultural Bioengineering, Ministry of Education, Center for R&D of Fine Chemicals of Guizhou University, Guiyang 550025, China.

出版信息

J Agric Food Chem. 2023 May 3;71(17):6525-6540. doi: 10.1021/acs.jafc.2c07810. Epub 2023 Apr 19.


DOI:10.1021/acs.jafc.2c07810
PMID:37073686
Abstract

As quorum sensing (QS) regulates bacterial pathogenicity, antiquorum sensing agents have powerful application potential for controlling bacterial infections and overcoming pesticide/drug resistance. Identifying anti-QS agents thus represents a promising approach in agrochemical development. In this study, the anti-QS potency of 53 newly prepared benzothiazole derivatives containing an isopropanolamine moiety was analyzed, and structure-activity relationships were examined. Compound exhibited the strongest antibacterial activity, with an EC of 1.54 μg mL against pv (). Compound suppressed QS-regulated virulence factors (e.g., biofilm, extracellular polysaccharides, extracellular enzymes, and flagella) to inhibit bacterial infection. anti- assays indicated good control efficiency (curative activity, 47.8%; protective activity, 48.7%) at 200 μg mL. Greater control efficiency was achieved with addition of 0.1% organic silicone or orange peel essential oil. The remarkable anti-QS potency of these benzothiazole derivatives could facilitate further novel bactericidal compound development.

摘要

群体感应(QS)调节细菌的致病性,因此抗群体感应剂在控制细菌感染和克服农药/药物抗性方面具有强大的应用潜力。因此,鉴定抗 QS 剂是农用化学品开发的一种很有前途的方法。在这项研究中,分析了 53 种新制备的含有异丙醇胺部分的苯并噻唑衍生物的抗 QS 效力,并研究了结构-活性关系。化合物 表现出最强的抗菌活性,对 pv ()的 EC 为 1.54 μg mL。化合物 抑制了 QS 调节的毒力因子(例如生物膜、胞外多糖、胞外酶和鞭毛),从而抑制细菌感染。抗 测定表明,在 200 μg mL 时具有良好的控制效率(治愈率为 47.8%;保护率为 48.7%)。添加 0.1%有机硅或橙皮精油可实现更高的控制效率。这些苯并噻唑衍生物的显著抗 QS 效力有助于进一步开发新型杀菌化合物。

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[6]
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[7]
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[8]
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