Table 1. Inhibitory activities of the type I and type II compounds against DNA gyrase from E. coli.
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Compound | Type | R1 | R2 | R3 | IC50 a (μM) or RA b (%) |
5 c | I | H | COOCH3 | — | IC50 = 88 ± 19 |
6 | I | H | CONHNH2 | — | RA = 100 |
7 | I | H | — | IC50 = 8.6 ± 2.4 | |
8 c | I | H | COOH | — | IC50 = 1.4 ± 0.2 |
14 | I | OBzl | COOCH3 | — | RA = 100 |
15 | I | OBzl | CONHNH2 | — | RA = 100 |
16 | I | OBzl | — | RA = 85 | |
17 | I | OBzl | COOH | — | IC50 = 0.86 ± 0.02 |
25 | II | — | — | COOCH3 | IC50 = 0.086 ± 0.011 |
26 | II | — | — | CONHNH2 | IC50 = 0.14 ± 0.02 |
27 | II | — | — | IC50 = 0.045 ± 0.022 | |
28 | II | — | — | COOH | IC50 = 0.020 ± 0.009 |
Novobiocin | IC50 = 0.17 ± 0.02 |
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