TABLE 3.
Antiparasitic activities of the studied compounds against C. parvum
| Series and compound | Log(P) | H2O solubility (ppm) | EC50 (μM [Ra]) | TC50b (μM [R]) |
|---|---|---|---|---|
| Series A | ||||
| 1 | 1.93 | 7.0 | 0.15 (0.99) | 3.9 (0.99) |
| 1a | −1.39 | 2,500.0 | —c | —d |
| 1b | −0.01 | 380.0 | 10.3 (0.97) | 9.7 (0.87) |
| 1c | −0.88 | 60.0 | 0.46 (0.87) | 25.5 (0.96) |
| 1d | 1.05 | 11.0 | 0.90 (0.97) | —d |
| 1e | 1.98 | 18.0 | 0.74 (0.97) | 85.9 (0.95) |
| 1f | 0.48 | 11.5 | 1.26 (0.76) | 36.6 (0.94) |
| 1g | 1.15 | 9.0 | 71.4 (0.96) | 153.0 (0.91) |
| Series B | ||||
| 2 | 4.41 | 5.0 | 0.13 (0.87) | —d |
| 2a | 0.84 | 1,290.0 | 11.3 (0.94) | 65.9 (0.94) |
| 2b | 2.22 | 137.0 | 6.5 (0.89) | 139.9 (0.88) |
| 2c | 1.60 | 10.0 | 6.16 (0.73) | —d |
| 2d | 3.53 | 2.4 | 2.1 (0.88) | —d |
| 2e | 4.46 | 2.6 | 0.67 (0.66) | 185 (0.92) |
| 2f | 2.96 | 10.0 | 1.39 (0.75) | —d |
| 2g | 3.63 | 6.0 | 0.12 (0.93) | —d |
| Series C | ||||
| 7a | 3.20 | NAe | 5.8 (0.98) | 93.1 (0.06) |
| 7b | 0.87 | NA | —c | —d |
| 7c | 0.93 | NA | 66.9 (0.86) | —d |
| 7d | 2.28 | NA | 7.2 (0.98) | 157 (0.95) |
| 7e | 2.55 | NA | 4.7 (0.98) | 96 (0.97) |
| 7f | 0.22 | NA | 49.5 (0.84) | 96 (0.97) |
a
R, confidence limits.
b
TC50, concentration at which 50% of the control cells are killed.
c
—, no activity detected at a concentration of 10 μM or less.
d
—, no toxic effects noted at the highest concentration tested (80 μM).
e
NA, not available.