Design,synthesis,and bioassay of 5-epi-aminoglycosides  

作　　者：YAN Ribai NIU Youhong LIU Yuheng DENG Junfeng YE Xinshan 

机构地区：[1]School of Pharmaceutical Sciences,Peking University,Beijing 100191,China [2]College of Pharmaceutical Science,Hebei Medical University,Shijiazhuang 050017,China [3]Antibiotics Research and Re-evaluation Key Laboratory of Sichuan Province,Sichuan Industrial Institute of Antibiotics,School of Pharmacy,Chengdu University,Chengdu 610106,China

出　　处：《Chinese Journal of Natural Medicines》2022年第11期854-862,共9页中国天然药物（英文版）

基　　金：supported by the National Natural Science Foundation of China(No.21877006).

摘　　要：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.

关 键 词：Antibiotic AMINOGLYCOSIDE A Site Structure-Activity Relationship 

分 类 号：R284[医药卫生—中药学]