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 ...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.展开更多
基金supported by the National Natural Science Foundation of China(No.21877006).
文摘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.
