Design, Synthesis, and Antibacterial Evaluation of Novel Isoindolin-1-ones Derivatives Containing Piperidine Fragments.

J Agric Food Chem

State Key Laboratory of Green Pesticide, Key Laboratory of Green Pesticide and Agricultural Bioengineering, Ministry of Education, Center for R&D of Fine Chemical of Guizhou University, Huaxi District Guiyang 550025, China.

Published: June 2024

A series of novel isoindoline-1-one derivatives containing piperidine moiety were designed and synthesized using natural compounds as raw materials, and their biological activities were tested for three bacterial and three fungal pathogens. These derivatives exhibited good against phytopathogenic bacteria activities against pv () and pv (). Some compounds exhibited excellent antibacterial activities against pv (). The dose of against (the maximum half lethal effective concentration (EC) = 21.3 μg/mL) was better than that of the thiediazole copper dose (EC = 53.3 μg/mL). Excitingly, further studies have shown that the molecular docking of with 2FBW indicates that it can fully locate the interior of the binding pocket through hydrogen bonding and hydrophobic interactions, thereby enhancing its anti- activity. Scanning electron microscopy (SEM) studies revealed that induced the cell membrane collapse. Moreover, the proteomic results also indicate that may be a multifunctional candidate as it affects the formation of bacterial biofilms, thereby exerting antibacterial effects.

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Source
http://dx.doi.org/10.1021/acs.jafc.3c09928DOI Listing

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