Further SAR exploring the role of chirality and substitution on the phenyl ring. IC50 values were determined against E. coli DNA gyrase in a supercoiling assay.
Compound | R 1 | R 2 | IC50a (μM) |
---|---|---|---|
28 | 76 | ||
29 | 36 | ||
30 | 180 | ||
31 | 41 | ||
32 | 45 | ||
33 | 41 | ||
34 | 62 | ||
35 | >200 |
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.