Table 1.
Antiprotozoal activity of the lapachol–triazole derivatives on Leishmania brazilensis (L. b) and Leishmania infantum (L. i) promastigotes, and T. cruzi epimastigotes and cytotoxicity on NCTC929 fibroblast cells.
| Compound | Leishmanicidal Activity (µM) |
Trypanocidal Activity (µM) | Cytotoxicity (µM) | Selectivity Index * | |||
|---|---|---|---|---|---|---|---|
| IC50—L. b | IC50—L. i | IC50 T. cruzi | CC50—L929 | L929/ L. b |
L929/ L. i |
L929/ T. cruzi |
|
| 1a | 10.7 | 24.9 | 19.2 | 106.4 | 10 | 4 | 6 |
| 1b | 6.7 | 30.5 | 37.3 | 128 | 19 | 4 | 3 |
| 2a | >256 | >256 | 68.7 | >256 | NE | NE | >4 |
| 3a | >256 | >256 | >256 | >256 | NE | NE | NE |
| 2b | >256 | >256 | 204.3 | >256 | NE | NE | >1 |
| 3b | >256 | >256 | >256 | >256 | NE | NE | NE |
| 2c | >256 | >256 | >256 | >256 | NE | NE | NE |
| 3c | >256 | >256 | >256 | >256 | NE | NE | NE |
| 2d | >256 | >256 | >256 | >256 | NE | NE | NE |
| 3d | >256 | >256 | >256 | >256 | NE | NE | NE |
| 2e | >256 | >256 | >256 | >256 | NE | NE | NE |
| 3e | >256 | >256 | >256 | >256 | NE | NE | NE |
| 2f | 14.5 | 38.2 | 21.1 | 31.8 | 2 | 1 | 2 |
| 3f | 17.6 | 46.6 | 24.7 | 312.2 | 18 | 7 | 13 |
| 2g | >256 | >256 | >256 | >384 | >2 | >2 | >2 |
| 3g | >256 | >256 | 146.5 | >384 | >2 | >2 | >3 |
| 2h | >256 | >256 | >256 | >256 | NE | NE | NE |
| 3h | >256 | >256 | >256 | >256 | NE | NE | NE |
| 2i | >256 | >256 | >256 | >256 | NE | NE | NE |
| 3i | >256 | >256 | >256 | >256 | NE | NE | NE |
| Miltefosine | 64.0 | 25.1 | NA | 2754 | 43.0 | 109.7 | NA |
| Benznidazole | NA | NA | 54.7 | 769 | NA | NA | 14.0 |
* SI = (CC50 L929/IC50 parasites); NA: not applicable; NE: not estimable; IC50 and CC50 values > 256 µM.