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. 2022 May 9;13(6):955–963. doi: 10.1021/acsmedchemlett.2c00111

Table 2. Target Inhibition by NBTIsa.

compd DNA gyrase IC50 (μM)b TopoIV IC50 (μM)c TopoIV/gyrase ratio
2a 0.047 (3) 0.54 (3) 11
3a 0.23 (2) 0.60 (2) 2.6
4a 0.23 (2) 1.7 (2) 7.6
2b 2.1 (2) 1.6 (2) 0.76
3b 0.58 (3) 2.9 (3) 5.0
2c 1.8 (3) 10 (2) 5.6
3c 1.7 (2) 7.4 (2) 4.4
3d 3.5 (2) 9.7 (2) 2.8
2e 4.2 (2) 1.4 (2) 0.33
3e 1.6 (2) 1.3 (5) 0.81
4e 0.19 (1) 1.1 (2) 5.8
2f 1.4 (2) 2.1 (2) 1.5
4f 0.15 (1) 0.42 (1) 2.8
gepotidacin (racemic) 0.17 (2) 2.8 (3) 16
ciprofloxacin 28 (2) 8.6 (2) 0.31
a

Average IC50 values from full concentration–response curves performed on separate days, with the number of replicate experiments in parentheses.

b

Inhibition of supercoiling activity.

c

Inhibition of decatenation activity.