Table 3.
Effect of C-7 ring structure on activity with G89C and D95Y GyrA variants of M. smegmatis
| Compound name | Compound typea | C-7 groupb | MIC ratio (89C/95Y)c |
|---|---|---|---|
| Moxifloxacin | Fluoroquinolone | a | 8 |
| PD161148 | Fluoroquinolone | b | 1 |
| UING5-248 | Fluoroquinolone | c | 2 |
| UING5-249 | Fluoroquinolone | d | 8 |
| UING5-47 | 2,4-Dione | a | 0.125 |
| UING5-48 | 2,4-Dione | b | 1 |
| UING5-63 | 2,4-Dione | c | 1 |
| UING5-200 | 2,4-Dione | d | 0.25 |
| UING5-157 | 3-NH2-2,4-dione | a | 0.062 |
| UING5-209 | 3-NH2-2,4-dione | b | 1 |
| UING5-159 | 3-NH2-2,4-dione | c | 0.2 |
| UING5-207 | 3-NH2-2,4-dione | d | 0.5 |
| UIJR1-100 | 1,3-Dione | d | 0.062 |
| UIJR-048 | 8-Me-2,4-dione | d | 0.062 |
a
8-Methoxy except for UIJR-048. Me, methyl.
b
The C-7 ring structures represented by the letters a through d are diagramed in Fig. 1.
c
Ratio of the MIC for the G89C mutant to that for the D95Y mutant.