Details

Autor(en) / Beteiligte

• Li, Jia‐Bao
• Xiong, Lan‐Tu
• Lu, Yan‐Rong
• Zhang, Yu‐Qing
• Xu, Xiao‐Li
• Wang, Hai‐Hong
• Deng, Xin
• Hu, Xu‐Hong
• Cui, Zi‐Ning

Titel

Novel pyrimidin‐4‐one derivatives as potential T3SS inhibitors against Xanthomonas campestris pv. campestris

Ist Teil von

• Pest management science, 2023-10, Vol.79 (10), p.3666-3675

Ort / Verlag

Chichester, UK: John Wiley & Sons, Ltd

Erscheinungsjahr

2023

Quelle

Wiley-Blackwell Journals

Beschreibungen/Notizen

• BACKGROUND Cruciferous black rot is caused by Xanthomonas campestris pv. campestris (Xcc) infection and is a widespread disease worldwide. Excessive and repeated use of bactericide is an important cause of the development of bacterial resistance. It is imperative to take new approaches to screening compounds that target virulence factors rather than kill bacterial pathogens. The type III secretion system (T3SS) invades a variety of cells by transporting virulence effector factors into the cytoplasm and is an attractive antitoxic target. Toward the search of new T3SS inhibitors, an alternative series of novel pyrimidin‐4‐one derivatives were designed and synthesized and assessed for their effect in blocking the virulence. RESULTS All of the target compounds were characterized by proton (1H) nuclear magnetic resonance (NMR), carbon‐13 (13C) NMR, fluorine‐19 (19F) NMR and high‐resolution mass spectrometry (HRMS). All compounds were evaluated using high‐throughput screening systems against Xcc. The results of the biological activity test revealed that the compound SPF‐9 could highly inhibit the activity of xopN gene promoter and the hypersensitivity (HR) of tobacco without affecting bacterial growth. Moreover, messenger RNA (mRNA) level measurements showed that compound SPF‐9 inhibited the expression of some representative genes (hrp/hrc genes). Compound SPF‐9 weakened the pathogenicity of Xcc to Raphanus sativus L. CONCLUSION Compound SPF‐9 has good potential for further development as a novel T3SS inhibitor against Xcc. © 2023 Society of Chemical Industry. Novel pyrimidin‐4‐one derivatives significantly inhibited Xanthomonas campestris pv. campestris (Xcc) type III secretion system (T3SS) and reduced the pathogenicity of Xcc to Raphanus sativus L.