Table 10.
In Vivo Efficacy of the Optimized Spiroindolones a
| Compound | 1 x 30 mg/kg | 3 x 30 mg/kg | ||||
|---|---|---|---|---|---|---|
| Activity (%) | Survival (Days) | Cure Rate (%) | Activity (%) | Survival (Days) | Cure Rate (%) | |
| 26 | 99.9 | 10.7 | 0 | 99.9 | 18.8 | 60 |
| 29 | 99.6 | 12.0 | 0 | 99.8 | 23.8 | 80 |
| 30b | 99.6 | 13.3 | 0 | 99.8 | 29.1 | 90 |
| CQ | 99.7 | 8.7 | 0 | 99.9 | 14.0 | 0 |
| AS | 92.2 | 7.3 | 0 | 99.0 | 11.8 | 0 |
a
average parasitemia reduction; survival of 6-7 days for untreated mice; cure was no parasites at day 30; compounds were formulated in 10% ethanol, 30% PEG400, 6% vitamin E TPGS;
b
formulated in 0.5% MCM / 0.1% Solutol HS15.