Table 4. Additional In Vitro Life Cycle Stage Profiling of the Most Potent Derivatives.
| oocyst
formation (% inhibition) |
||||
|---|---|---|---|---|
| Cpd | male gamete inhibition % | female gamete inhibition % | TRAa | TBAb |
| 1 | 72.98 ± 5.97c | 51.74 ± 5.40c | 76.0 ± 4.75c | 36.0 ± 10.6c |
| 2 | 95.45 ± 4.55 | 78.88 ± 4.46 | nd | nd |
| 3 | 81.36 ± 8.64 | 67.05 ± 0.39 | 11 | 36 |
| 4 | 43.94 ± 10.61 | 74.48 ± 2.26 | nd | 26 |
| 5 | 48.01 ± 24.82 | 61.03 ± 14.35 | 38 | 63 |
| 6 | 34.59 ± 14.27 | 64.59 ± 12.33 | 53 | 67 |
| 7 | 27.14 ± 14.02 | 34.05 ± 9.23 | nd | nd |
| 8 | 23.51 ± 9.72 | 54.00 ± 2.54 | nd | nd |
| 9 | 96.67 ± 3.33 | 90.50 ± 7.17 | 70 | 47 |
| 13 | 90.91 ± 9.09 | 87.02 ± 3.68 | 70 | 64 |
| 19 | 95.45 ± 4.55 | 86.30 ± 2.58 | 47 | 36 |
| 20 | 95.0 ± 5.00 | 77.52 ± 10.85 | 75 | 54 |
| 21 | 95.45 ± 4.55 | 86.30 ± 2.58 | 56 | 20 |
| 22 | 92.12 ± 1.21 | 85.40 ± 7.62 | 89 | 80 |
a
Transmission-reducing activity (TRA) after a 48 h drug treatment at 2 μM, of a single biological repeat.
b
Transmission-blocking activity (TBA) after a 48 h drug treatment at 2 μM, of a single biological repeat.
c
Published in Reader et al.4 nd–not determined.