Home Journals Articles Updates About
CN
image
收藏切换
Synthesis of ornithine peptidomimetic efflux pump inhibitors and synergistic antibiotic activity against Pseudomonas aeruginosa
收藏切换
PDF
Xi ZHU, Xi-can MA, Xin-tong ZHANG, Yi-shuang LIU, Ning HE, Yun-ying XIE, Dan-qing SONG*
Acta Pharmaceutica Sinica | 2024, 59(6) : 1720 - 1729
Less
收藏切换
Acta Pharmaceutica Sinica | 2024, 59(6): 1720-1729
• Original Articles •
Synthesis of ornithine peptidomimetic efflux pump inhibitors and synergistic antibiotic activity against Pseudomonas aeruginosa
Full
Xi ZHU, Xi-can MA, Xin-tong ZHANG, Yi-shuang LIU, Ning HE, Yun-ying XIE, Dan-qing SONG*
Affiliations
  • Institute of Medicinal Biotechnology, Chinese Academy of Medical Sciences and Peking Union Medical College, Beijing 100050, China
Published: 2024-06-12 doi: 10.16438/j.0513-4870.2024-0104
Outline
收藏切换

In order to solve the problem of resistance of Pseudomonas aeruginosa to multiple antibiotics, it is an effective way to find inhibitors of P.aeruginosa efflux pump. In this study, 15 new ornithine peptidomimetic derivatives were designed and synthesized by changing the side chain structure of natural amino acids with PAβN, a dipeptide efflux pump inhibitor, and their synergic activity with aztreonam, a monocyclic β-lactam antibiotic, against P.aeruginosa was evaluated. Among them, the representative compound 12b not only enhanced the antibacterial activity of β-lactam antibiotics aztreonam, ceftazidime and meropenem, but also significantly enhanced the antibacterial action of macrolide antibiotics clarithromycin, showing a broad-spectrum synergic sensitization effect. In addition, compound 12b also has a good safety. Preliminary mechanisms suggest that 12b works by directly targeting the efflux transporter MexB. These results provide a new lead compound for the development of a new class of efflux pump inhibitors against P.aeruginosa.

efflux pump inhibitor  /  synthesis  /  Pseudomonas aeruginosa  /  synergistic activity  /  MexAB-OprM
Xi ZHU, Xi-can MA, Xin-tong ZHANG, Yi-shuang LIU, Ning HE, Yun-ying XIE, Dan-qing SONG. Synthesis of ornithine peptidomimetic efflux pump inhibitors and synergistic antibiotic activity against Pseudomonas aeruginosa[J]. Acta Pharmaceutica Sinica, 2024 , 59 (6) : 1720 -1729 . DOI: 10.16438/j.0513-4870.2024-0104
Appendix
Less
Year 2024 volume 59 Issue 6
PDF
208
87
Cite this Article
BibTeX
Article Info
doi: 10.16438/j.0513-4870.2024-0104
  • Receive Date：2024-02-01
  • Online Date：2025-11-26
  • Published：2024-06-12
Article Data
Affiliations
History
  • Received：2024-02-01
  • Revised：2024-03-15
Funding
Affiliations
    Institute of Medicinal Biotechnology, Chinese Academy of Medical Sciences and Peking Union Medical College, Beijing 100050, China
References
Share
https://castjournals.cast.org.cn/joweb/yxxb/EN/10.16438/j.0513-4870.2024-0104
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