Biphenyl inhibitors with further biological evaluation reported. 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.
Compound | R | Ring chirality | E. coli DNA gyrase IC50 (μM) | E. coli topo IV IC50 (μM) | E. coli K12 MG1655 MIC (μg mL−1) | S. aureus NCIMB 50080 MIC (μg mL−1) | E. coli K12 MG1655 S83L MIC (μg mL−1) |
---|---|---|---|---|---|---|---|
Ciprofloxacinb | 0.6 | 5.7 | 0.016 | 0.5 | 0.5 | ||
1 | Thiophene | 0.3a | >540a | 8a | 8a | N.D. | |
5 | (R) | 21 | >100 | 32 | 16 | 32 | |
6 | (R) | 12 | >100 | 64 | 32 | 64 | |
7 | (R) | 17 | 64 | 32 | 16 | 32 | |
11 | (R) | 73 | 94 | >128 | >128 | >128 | |
31 | Racemic (3-OH) | 41 | >100 | >128 | 128 | >128 |
Data from ref. 14 which used different E. coli and S. aureus bacterial strains.
Ciprofloxacin used as a standard control.