Synthesis and biological evaluation of stilbene‐based peptoid mimics against the phytopathogenic bacterium Xanthomonas citri pv. citri. Issue 1 (24th September 2020) - Li, Yan
Abstract: BACKGROUND: The emergence of drug‐resistant phytopathogenic bacteria and the need for new types of biological disease‐control agents have accelerated efforts toward searching for alternative candidates with a low propensity for resistance development. In this study, a new series of stilbene‐based peptoid mimics were synthesized, and their biological activities were evaluated against citrus pathogenic bacteria in vitro and in vivo . RESULTS: Antibacterial bioassay results showed that the dicationic peptoid mimics 9a and 9b displayed excellent bioactivity against Xanthomonas citri pv. citri, with the minimum inhibitory concentration values of 25 μM, which were superior to those of commercial copper biocides Delite (200 μM) and Kasumin Bordeaux (100 μM). In vivo bioassay further confirmed their control efficacy against plant bacterial diseases. In addition, the antibacterial mechanism of action elucidated their membrane‐disruption effects resulting in the leakage of the bacterial membranes, which was similar to that of antimicrobial peptides. Moreover, the inhibition effect on biofilm formation of peptoid mimics has also been demonstrated. CONCLUSION: Stilbene‐based peptoid mimics synthesized in this study showed promising antibacterial activity with a potent membrane‐disruptive mechanism. The results suggested that stilbene‐based peptoid mimics have the potential as a candidate new type of bactericide for citrus disease protection. Abstract : Dicationic peptoid mimics killed Xanthomonas citri pv. citri by inducing membrane leakage, preferentially targeting bacterial membranes. © 2020 Society of Chemical Industry