Design, synthesis, antimicrobial activity, and mechanism of novel 3‐(2,4‐dichlorophenyl)‐[1,2,4]triazolo[3,4‐b][1,3,4]thiadiazole derivatives

Author:

Zheng Yuguo12,Chen Mei2,Zhang Renfeng2,Xue Wei1ORCID

Affiliation:

1. State 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 China

2. The Key Laboratory of Chemical Synthesis and Environmental Pollution Control‐Remediation Technology of Guizhou Province, Minzu Normal University of Xingyi Xingyi China

Abstract

AbstractBACKGROUNDPlant pathogens cause substantial crop losses annually, posing a grave threat to global food security. Fungicides have usually been used for their control, but the rapid development of pesticide resistance renders many ineffective, therefore the search for novel and efficient green pesticides to prevent and control plant diseases has become the top priority in crop planting.RESULTSThe results of bioassay studies indicated that most of the target compounds showed certain antimicrobial activity in vitro. In particular, compound X7 showed high inhibitory activity against Xanthomonas oryzae pv. oryzae (Xoo), with an EC50 value of 27.47 μg mL−1, surpassing conventional control agents such as thiazole zinc (41.55 μg mL−1) and thiodiazole copper (53.39 μg mL−1). Further studies on molecular docking showed that X7 had a strong binding affinity with 2FBW. The morphological change observed by scanning electron microscopy indicated that the surface of Xoo appears wrinkled and cracked under X7 treatment and a total of 2662 proteins were identified by label‐free proteomic analysis. Three experiments have elucidated the mechanism whereby X7 induced considerable changes in the physiological and biochemical properties of Xoo, which in turn affected the reproduction and growth of bacteria.CONCLUSIONThis work represents a pivotal advancement, offering important reference for the research and development therapeutics in combating plant pathogens. © 2024 Society of Chemical Industry.

Publisher

Wiley

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