Table 6. In Vivo Efficacy of Acetamide Pyrrolidines in P. chabaudi ASS Infected Mice.
| Plasma
Compound Concentration (nM)b |
||||
|---|---|---|---|---|
| Oral Dose (qd) | % Inh. of Growtha | 1 h | 6 h | 24 h |
| 30a, 10 mg/kg/day | 61.2 ± 6.6 | 255 ± 60 | 181 ± 55 | 7.4 ± 4.2 |
| 31a, 10 mg/kg/day | 65.3 ± 11.3 | 129 ± 22 | 119 ± 56 | 14.9 ± 7.0 |
| 32a, 3 mg/kg/day | 34.0 ± 16.7 | 114 ± 21 | 34.1 ± 5.0 | 6.6 ± 2.0 |
| 32a, 10 mg/kg/day | 94.1 ± 1.5 | 389 ± 148 | 48.9 ± 4.0 | 1.7 ± 0.3 |
| 32a, 30 mg/kg/day | 99.9 ± 0.0 | 1310 ± 420 | 1150 ± 500 | 28.5 ± 20.4 |
| CQ, 10 mg/kg/day | 99.9 ± 1.1 | 80.7 ± 9.6 | 83.4 ± 8.9 | 68.6 ± 12.0 |
a
Inhibition of parasitemia after 4 days of qd oral dosing.
b
Plasma compound concentrations were determined at the designated hour post dosing on day 4. n = 6 animals/group. nd = not determined.