In vitro data for the novel biphenyl series of DNA gyrase inhibitors designed to investigate the SAR and hydrophobic and steric requirements of the E. coli DNA gyrase allosteric site.
| |||||
|---|---|---|---|---|---|
| Compound | R | IC50a (μM) | Compound | R | IC50a (μM) |
| 2 |
|
60 | 9 |
|
35 |
| 3 |
|
20 | 10 |
|
39 |
| 4 |
|
20 | 11 |
|
73 |
| 5 |
|
21 | 12 |
|
42 |
| 6 |
|
12 | 13 |
|
24 |
| 7 |
|
17 | 14 |
|
41 |
| 8 |
|
46 | 15 | Br | >200 |
a
IC50 values were the mean of 2 or 3 different experiments. Error limits are not given, as the gel-based assays used are at best semi-quantitative.