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

查看全文 作　　者：YAN [1]Ribai;NIU [1]Youhong;LIU [2]Yuheng;DENG [3]Junfeng;YE [1]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》索引2022年第20卷第11期,共9页 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