Home Journals Articles Updates About
CN
image
收藏切换
Design, synthesis, and in vitro antibacterial activity evaluation of nitroimidazole derivatives against intestinal pathogenic Fusobacterium nucleatum
收藏切换
PDF
Yu-ping CHEN1, Feng CHEN1, 2, Shan-chao WU1, *
Acta Pharmaceutica Sinica | 2025, 60(5) : 1464 - 1473
Less
收藏切换
Acta Pharmaceutica Sinica | 2025, 60(5): 1464-1473
• Original Articles •
Design, synthesis, and in vitro antibacterial activity evaluation of nitroimidazole derivatives against intestinal pathogenic Fusobacterium nucleatum
Full
Yu-ping CHEN1, Feng CHEN1, 2, Shan-chao WU1, *
Affiliations
  • 1. The Center for Basic Research and Innovation of Medicine and Pharmacy (MOE), School of Pharmacy, Second Military Medical University (Naval Medical University), Shanghai 200433, China
  • 2. College of Pharmacy, Dali University, Dali 671000, China
Published: 2025-05-12 doi: 10.16438/j.0513-4870.2025-0358
Outline
收藏切换

Fusobacterium nucleatum (Fn) is closely associated with the occurrence and progression of colorectal cancer (CRC). The development of specific antibacterial agents targeting Fn is crucial for the prevention and treatment of CRC. Based on the preliminary phenotypic screening results from our research group, dimetridazole was successfully identified as a hit compound with antibacterial activity against Fn. In this preliminary structural optimization study, we designed and synthesized seven novel nitroimidazole derivatives comprising three structural types, followed by antimicrobial evaluation of all target compounds. Among them, compound CL6 exhibited excellent antibacterial activity against Fn (MIC = 0.5 μg·mL-1) and demonstrated good selectivity towards intestinal bacteria and normal cells. Compound CL6 significantly inhibited the migration of CRC cells (HCT116) induced by Fn preliminary mechanistic studies suggest that compound CL6 disrupts the integrity of the Fn bacterial biofilm and cell wall, providing a promising lead compound for the development of novel anti-Fn drugs.

Fusobacterium nucleatum  /  colorectal cancer  /  dimetridazole  /  antibacterial activity  /  mechanism
Yu-ping CHEN, Feng CHEN, Shan-chao WU. Design, synthesis, and in vitro antibacterial activity evaluation of nitroimidazole derivatives against intestinal pathogenic Fusobacterium nucleatum[J]. Acta Pharmaceutica Sinica, 2025 , 60 (5) : 1464 -1473 . DOI: 10.16438/j.0513-4870.2025-0358
Appendix
Less
Year 2025 volume 60 Issue 5
PDF
332
143
Cite this Article
BibTeX
Article Info
doi: 10.16438/j.0513-4870.2025-0358
  • Receive Date：2025-04-01
  • Online Date：2025-10-29
  • Published：2025-05-12
Article Data
Affiliations
History
  • Received：2025-04-01
  • Revised：2025-04-11
Funding
Affiliations
    1. The Center for Basic Research and Innovation of Medicine and Pharmacy (MOE), School of Pharmacy, Second Military Medical University (Naval Medical University), Shanghai 200433, China
    2. College of Pharmacy, Dali University, Dali 671000, China
References
Share
https://castjournals.cast.org.cn/joweb/yxxb/EN/10.16438/j.0513-4870.2025-0358
Share to
QR

Scan QR to access full text

Cite this article
BibTeX
Citations
表12种不同金属材料的力学参数
科
Family		 属数
Number of
genus		 种数
Number of
species		 占总种数比例
Percentage of
total species (%)		 属
Genus		 种数
Number of
species		 占总种数比例
Percentage of total
species (%)
鹅膏菌科Amanitaceae 2 11 5.26 鹅膏菌属 Amanita 10 4.78
小菇科 Mycenaceae 2 12 5.74 丝盖伞属 Inocybe 5 2.39
多孔菌科 Polyporaceae 8 14 6.70 蜡蘑属 Laccaria 5 2.39
红菇科 Russulaceae 3 23 11.00 小皮伞属 Marasmius 6 2.87
小菇属 Mycena 11 5.26
光柄菇属 Pluteus 5 2.39
红菇属 Russula 17 8.13
栓菌属 Trametes 5 2.39
关闭全屏
  • BibTeX
  • EndNote
  • RefWorks
  • TxT
Links
Articles
Latest Articles
Most Read
Collections
Updates
Events
News
Multimedia
About
About Us
Contact
No. 86 Xueyuan South Road, Haidian District, Beijing
100081
010-62199257
qkjq@cast.org.cn

Copyright © 2025 China Association for Science and Technology. All rights reserved. For all open access content, the relevant licensing terms apply.
Sponsored by the Office of the Leading Group for Cybersecurity and Informatization of CAST, and supported by Science and Technology Review Publishing House