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Structure-activity relationships of neomycin analogues related to binding and inhibition of Escherichia coli rRNA synthesis.
We have synthesized and characterized a series of neomycin analogues which vary in their length of aglycon and/or D-glycero-D-galacto backbone, in which a methyl group is replaced by amine, hydroxyl, ester, aminoacyl, and fatty acid groups. We tested these compounds for binding to the rRNA promoter in vitro and for inhibition of rRNA synthesis in vivo. In addition, we determined the minimum inhibitory concentrations (MICs) of these compounds for a broad panel of Gram-negative and Gram-positive bacteria, including both non-beta-lactam-susceptible and beta-lactam-resistant strains. The results of these experiments indicate that the neomycin A ring structure is primarily responsible for the antibacterial activity of neomycin compounds, whereas the choice of aliphatic or heterocy

https://colab.research.google.com/drive/1Taf91lT9C6moP7g61CZmLiXcLdAEvpZW
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