TABLE 6.
Activities of compounds against intracellular T. cruzi amastigotes, bloodstream form of Trypanosoma brucei rhodesiense, and Plasmodium falciparum cultured in red blood cellsa
| Compound | IC50 (μM)
|
||
|---|---|---|---|
| T. cruzi | T. b. rhodesiense | P. falciparum | |
| 1a | >151 | 16.0 | 0.8 |
| 1b | 1.8 | 0.7 | 3.1 |
| 1c | 2.8 | 0.5 | 0.9 |
| 1d | >132 | 13.1 | >22 |
| 1e | >111 | 12.5 | 14.2 |
| 1f | 30.2 | 10.3 | 10.0 |
| 1g | 46.0 | 5.5 | 12.3 |
| 2a | 130 | 60.6 | 5.4 |
| 2b | 4.7 | 0.7 | 2.8 |
| 2c | 25.4 | 2.5 | 1.8 |
| 3a | 16.0 | 35.1 | 11.6 |
| 3b | 23 | 7.2 | 14 |
| 3c | 16.3 | 2.1 | 4.1 |
| 3d | 3.1 | 1.1 | 4.8 |
| 3e | 34.1 | 24.2 | 11.0 |
| 3f | 51.1 | 22.4 | 15.0 |
| 3g | 10.2 | 2.2 | 9.0 |
| 3h | 61.3 | 17.1 | 6.2 |
| 3i | 64.2 | 5.6 | 12.0 |
| 4a | 5.6 | 3.3 | 4.0 |
| 4b | 90.2 | 146.3 | >18.4 |
| 4c | 90.4 | 53.0 | 18.7 |
| 4d | 67.2 | 18.4 | 8.2 |
| 4e | 18.9 | 9.2 | 4.3 |
| 4f | >131 | 173 | 18.9 |
| 4g | 25.6 | 257.8 | 10.0 |
| 4h | 26.2 | 19.9 | 7.1 |
| 4i | 97 | 5.7 | >21 |
| 4j | >114 | 53.3 | 9.3 |
| 4k | 44.9 | 30.8 | 10.9 |
| 4l | >117 | 62.4 | 11.7 |
| 4n | 72.6 | 30.3 | 10.2 |
| 4p | 21.2 | 5.4 | 5.9 |
| 4q | 5.6 | 0.5 | 0.7 |
| 4r | 9.6 | 1.9 | 1.9 |
| 4s | 13.4 | 3.4 | 2.0 |
| 5a | 25.6 | 14.5 | 6.5 |
| 5b | 8.2 | 12.8 | 3.3 |
| 5c | 5.8 | 0.5 | 1.4 |
| 5d | 5.6 | 1.2 | 0.6 |
| 5e | 5.3 | 1.4 | 3.0 |
| 5f | 4.7 | 1.1 | 2.1 |
| 5g | 33.8 | 10.9 | 2.7 |
| 5h | 19.1 | 7.1 | 1.7 |
| 5i | 18.8 | 3.8 | 1.1 |
| 5j | 19.4 | 1.7 | 0.6 |
| 5k | 3.1 | 1.2 | 1.1 |
| 5l | 3.4 | 1.2 | 0.6 |
| 5m | 22.9 | 32.3 | 5.2 |
| 5n | 50 | 64.7 | 5.0 |
a
The control compounds were benznidazole (IC50 = 1.36 μM) for T. cruzi, melarsoprol (IC50 = 0.008 μM) for T. b. rhodesiense, and chloroquine (IC50 = 0.083 μM) for P. falciparum.