Table 1.
MIC of C-2 and C-3 modified quinolones in E. coli and M. smegmatis.
| Compound | C-2 | C-3 | C-7 | Bacterial Strain (MIC μg/mL) |
||
|---|---|---|---|---|---|---|
| E. colia | E. coli tolCb | M. smegmatisc | ||||
| Ciprofloxacin | H | CO2H | Piperazinyl | 0.04 | 0.008 | 0.156 |
| 13 | H | H | Piperazinyl | 50 | 1.56 | 6.25 |
| Ulifloxacin | Thiazetidine | CO2H | Piperazinyl | 0.062 | 0.016 | 3.13 |
| 15 | Thiazetidine | H | Piperazinyl | >200 | 200 | 200 |
| Moxifloxacin | H | CO2H | octahydropyrrolopyridinyl | 0.156 | 0.004 | 0.08 |
| 11 | H | H | octahydropyrrolopyridinyl | >200 | 100 | >200 |
| 7a | S-ethyl | CO2H | Piperazinyl | 200 | 12.5 | >200 |
| 7b | S-ethyl | CO2H | octahydropyrrolopyridinyl | >50 | >50 | 50 |
| 9a | S-ethyl | H | Piperazinyl | >50 | 25 | >50 |
| 9b | S-ethyl | H | octahydropyrrolopyridinyl | >200 | 100 | >200 |
| 9c | S-isopropyl | H | Piperazinyl | >50 | >50 | >50 |
| 9d | S-isopropyl | H | octahydropyrrolopyridinyl | >50 | 50 | 50 |
KD65
KD1397
KD1163