Table 9.
Antiparasitic activity of select compounds. Assays as described in Methods18. Unless otherwise stated all values are the average of three independent determinations.
| Compound | EC50 (μM) | Selectivitya | |
|---|---|---|---|
| Toxo/WT | Toxo/CpIMPDH | ||
| 1 | 1.3 ± 0.1 b | 0.65 ± 0.03 b | 2 |
| 26 | 9 ± 3 | 9 ± 3 | 1 |
| 40a | 3 ± 1 | 0.02 ± 0.02 | 150 |
| 41 | 3.0 ± 1.0 | 0.9 ± 0.4 | 3 |
| 43 | 7 ± 4 | 4 ± 2 | 2 |
| 44 | >25 | 0.5 ± 0.2 | >50 |
| 45 | 1.1 ± 0.4 | 0.5 ± 0.1 | 2 |
| 46 | 8 ± 2 | 0.22 ± 0.04 | 40 |
| 48 | 2.4 ± 0.3 | 0.20 ± 0.09 b | 34 |
| 54 | 2.2 ± 0.6 | 0.4 ± 0.3 | 5 |
| 55 | 5 ± 2 | 0.3 ± 0.1 | 16 |
| 56 | 1.7 ± 0.6 | 0.8 ± 0.4 | 2 |
| 57 | 3 ± 1 | 0.19 ± 0.03 | 14 |
| 58 | 21 ± 6 | 0.7 ± 0.1 | 30 |
| 62 | 3.3 ± 0.5 | 0.2 ± 0.01 | 15 |
| 63 | 3.2 ± 0.8 | 0.30 ± 0.3 | 11 |
| 64 | 5 ± 4 | 2 ± 2 | 3 |
| 65 | 2.2 ± 0.8 | 0.3 ± 0.1 | 7 |
| 66 | 1.7 ± 0.7 | 1.0 ± 0.1 | 1.7 |
| 70 | 5 ± 3 | 2.5 ± 0.2 | 1.9 |
| 72 | 2.1 ± 0.5 | 0.4 ± 0.1 | 5 |
| 73 | 4 ± 2 | 0.02 ± 0.02 | 200 |
a
Selectivity is the ratio of EC50 Toxo/CpIMPDH to EC50 Toxo/WT.
b
Two determinations.