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It is urgent to develop new antibacterial molecules with low toxicity and high efficiency. Marinoquinoline A is an alkaloid isolated from marine actinomycetes and has a variety of pharmacological activities. In this study, a series of compounds were designed and synthesized by fragment fusion strategy inspired by Marinoquinoline, and their antibacterial activities were evaluated, and the structure\u2013activity relationship was discussed.<\/jats:p><\/jats:sec><jats:sec><jats:title>RESULTS<\/jats:title><jats:p>Among these derivatives, <jats:bold>ZM\u20109<\/jats:bold> showed the most significant antibacterial activity against <jats:italic>Xanthomonas oryzae<\/jats:italic> (<jats:italic>Xoo<\/jats:italic>) with MIC of 1.56\u2009\u03bcg\u2009mL<jats:sup>\u22121<\/jats:sup>, while <jats:bold>ZN\u20108<\/jats:bold> showed the best antibacterial activity against <jats:italic>Xanthomonas axonopodis<\/jats:italic> pv. <jats:italic>Citri<\/jats:italic> (<jats:italic>Xac<\/jats:italic>) with MIC of 0.78\u2009\u03bcg\u2009mL<jats:sup>\u22121<\/jats:sup>, both of which were better than Thiodiazole copper. The results of <jats:italic>in vivo<\/jats:italic> antibacterial activity test showed that 200\u2009\u03bcg\u2009mL<jats:sup>\u22121<\/jats:sup> <jats:bold>ZM\u20109<\/jats:bold> and <jats:bold>ZN\u20108<\/jats:bold> had significant control effects on rice and citrus. The biochemical experiments showed that <jats:bold>ZM\u20109<\/jats:bold> and <jats:bold>ZN\u20108<\/jats:bold> could inhibit the secretion of extracellular polysaccharides, destroy the biofilm integrity of the pathogens, increase permeability, and cause oxidative stress damage.<\/jats:p><\/jats:sec><jats:sec><jats:title>CONCLUSION<\/jats:title><jats:p>In summary, most of the chemical entities inspired by Marinoquinoline have shown good antibacterial activity. In particular, compounds <jats:bold>ZM\u20109<\/jats:bold> and <jats:bold>ZN\u20108<\/jats:bold> can be used as lead compounds for further structural optimization to develop new antibacterial agents. \u00a9 2024 Society of Chemical Industry.<\/jats:p><\/jats:sec>","DOI":"10.1002\/ps.8609","type":"journal-article","created":{"date-parts":[[2024,12,28]],"date-time":"2024-12-28T00:30:32Z","timestamp":1735345832000},"page":"2086-2100","update-policy":"https:\/\/doi.org\/10.1002\/crossmark_policy","source":"Crossref","is-referenced-by-count":2,"title":["Design, synthesis and antimicrobial activity evaluation of novel Marinoquinoline derivatives against phytopathogenic bacteria"],"prefix":"10.1002","volume":"81","author":[{"ORCID":"https:\/\/orcid.org\/0009-0003-8657-4645","authenticated-orcid":false,"given":"Han","family":"Zhou","sequence":"first","affiliation":[{"name":"School of Pharmacy Lanzhou University  Lanzhou 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