Table 2. Inhibitory activities of selected compounds against DNA gyrase from S. aureus and topoisomerase IV from E. coli and S. aureus.
Compound | IC50
a
(μM) or RA
b
(%) |
||
S. aureus DNA gyrase | E. coli topoisomerase IV | S. aureus topoisomerase IV | |
8 c | RA = 88 | RA = 91 | RA = 100 |
17 | RA = 87 | RA = 84 | RA = 92 |
25 | IC50 = 63 ± 14 | RA = 72 | RA = 100 |
26 | RA = 80 | RA = 88 | RA = 98 |
27 | IC50 = 11 ± 2 | RA = 91 | RA = 60 |
28 | IC50 = 1.4 ± 0.4 | IC50 = 11 ± 3 | IC50 = 14 ± 4 |
Novobiocin | IC50 = 0.041 ± 0.007 | IC50 = 11 ± 2 | IC50 = 27 ± 7 |
aConcentration of compound that inhibits the enzyme activity by 50%.
bResidual activity of the enzyme at 10 μM concentration of the compound.
cPreviously published results.20