Table 10. In Vivo Efficacy of Selected Analogues on Plasmodium Mouse Malaria Modelsa.
| parameters | 2 |
3 |
|
|---|---|---|---|
| malaria model | P. berghei | P. berghei | P. falciparum |
| dose (mg/kg) | 1 × 100 | 1 × 100 | 4 × 25 |
| activity (%) | 94 | 99 | >99.9 |
| survival (days) | 6 | 7 | |
| Cmax (μM) | 13.1 | 20.6 | 5.2 |
| AUC (μM h) | 165.4 | 377.1 | 86.0 |
a
Activity = average parasitemia reduction compared with untreated controls; survival = average lifespan after infection (6–7 days for untreated control mice); Cmax = maximum concentration of drug in plasma; AUC = area under the curve; compounds were formulated in 0.5% methyl cellulose/0.5% Tween 80 in water for oral administration.