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. 2016 Feb 8;7(4):418–423. doi: 10.1021/acsmedchemlett.6b00006

Table 1. Comparative Antibacterial Activity and Inhibition of Translation in Eukaryotic and Prokaryotic Systemsa.

  translation inhibitionb
antibacterial activity MIC (μM)c
compd IC50Euk (μM) IC50Pro (μM) E. coli R477/100 B. subtilis ATCC6633
Genta. 62 ± 9 0.03 ± 0.00 6 <0.75
G418 2.0 ± 0.3 0.01 ± 0.00 9 <1.25
1 347.1 ± 34.3 6.0 ± 1.0    
(R)-4 120.5 ± 14.5 11.0 ± 1.2 >311 311
(S)-5 515.8 ± 15 91.9 ± 8.4 >375 >375
2 13.9 ± 1.2 1.0 ± 0.1 680 42
6 7.5 ± 0.5 0.7 ± 0.1 >273 34
3 1.5 ± 0.1 1.1 ± 0.2 1267 156
7 1.2 ± 0.1 1.2 ± 0.1 >257 64
a

In all biological tests, all AGs were in their sulfate salt forms, and the concentrations refer to the free amine form of each AG.

b

The eukaryotic and prokaryotic half-maximal-inhibition values (IC50Euk and IC50) were quantified in coupled transcription/translation assays by using active luciferase detection as previously described by us.5

c

Minimal inhibitory concentration (MIC) values were determined by using the double-microdilution method.