Design, synthesis, and bioassay of 5-epi-aminoglycosides.
10.1016/S1875-5364(22)60212-7
- Author:
Ribai YAN
1
;
Youhong NIU
2
;
Yuheng LIU
3
;
Junfeng DENG
4
;
Xinshan YE
5
Author Information
1. School of Pharmaceutical Sciences, Peking University, Beijing 100191, China. Electronic address: yanribai@bjmu.edu.cn.
2. School of Pharmaceutical Sciences, Peking University, Beijing 100191, China.
3. College of Pharmaceutical Science, Hebei Medical University, Shijiazhuang 050017, China.
4. Antibiotics Research and Re-evaluation Key Laboratory of Sichuan Province, Sichuan Industrial Institute of Antibiotics, School of Pharmacy, Chengdu University, Chengdu 610106, China.
5. School of Pharmaceutical Sciences, Peking University, Beijing 100191, China. Electronic address: xinshan@bjmu.edu.cn.
- Publication Type:Journal Article
- Keywords:
A Site;
Aminoglycoside;
Antibiotic;
Structure-Activity Relationship
- MeSH:
Aminoglycosides/chemistry*;
Anti-Bacterial Agents/chemistry*;
RNA, Ribosomal, 16S/metabolism*;
Structure-Activity Relationship;
Biological Assay
- From:
Chinese Journal of Natural Medicines (English Ed.)
2022;20(11):854-862
- CountryChina
- Language:English
-
Abstract:
For the purpose of seeking new antibiotics, researchers usually modify the already-existing ones. However, this strategy has been extensively used and is close to its limits, especially in the case of aminoglycosides, and it is difficult to find a proper aminoglycoside antibiotic for novel modification. In this paper, we reported the design, synthesis, and evaluation of a series of 5-epi-neamine derivatives based on the structural information of bacterial 16S RNA A-site binding with aminoglycosides. Bioassay results showed that our design strategy was feasible. Our study offers a new way to search for structurally novel aminoglycosides. Meanwhile, our study provides valuable structure-activity relationship information, which will lead to better understanding and exploitation of the drug target, and improved development of new aminoglycoside antibiotics.
