Table 3. Mice in Vivo Efficacy and IV PK.
| compd | Sa1118 MIC (μg/mL) | septicemia efficacy PD50 (mg/kg) | Spn MIC (μg/mL) | lung efficacy ED-2log/ED-3log (mg/kg) | DNAUCa (μg·h/mL)/(mg/kg) | Vdss (L/kg) | t1/2 (h) | Cl (mL/min/kg) |
|---|---|---|---|---|---|---|---|---|
| Novobiocin | 0.125 | 10 | 2 | >100/>100 | ND | ND | ND | ND |
| 2 | 0.06 | 1 | 0.06 | >25/>25c | 0.159 | 3.47 | 2.1 | 105 |
| 22 | 0.125 | NDb | 0.25 | 63.0/97.6 | 0.397 | 1.70 | 2.0 | 42 |
| 31 | 0.125 | ND | 0.125 | 60.6/103.7 | 0.893 | 0.32 | 0.31 | 19 |
| Moxifloxacin | ND | ND | 0.06 | 28.6/50.8 | ND | ND | ND | ND |
a
Mice were dosed IV at 2 mg/kg.
b
Not determined.
c
The highest achievable IV dose due to the solubility limitation.