Table 1.
Activity against promastigotes and intracellular amastigotes of Leishmania amazonensis, cytotoxicity in BALB/c peritoneal macrophages, and selectivity index after 24 h of treatment with 1,4-disubstituted-1,2,3-triazole compounds.
| Compounds | IC50 (µM) | CC50 (µM) | SI | |
|---|---|---|---|---|
| Promastigote | Intracellular Amastigote | |||
| 1 | 53.70 ± 8.467 | – | 221.20 ± 4.824 | – |
| 2 | 8.85 ± 3.436 | 37.92 ± 3.350 | 248.46 ± 2.519 | 6.55 |
| 3 | 50.93 ± 4.571 | – | 307.73 ± 4.071 | – |
| 4 | 15.68 ± 5.418 | 149.8 ± 6.367 | 144.80 ± 4.100 | 0.96 |
| 5 | 8.81 ± 3.933 | 32.31 ± 2.256 | 58.01 ± 2.647 | 1.79 |
| 6 | 14.64 ± 4.392 | 17.78 ± 3.257 | 547.88 ± 3.256 | 30.81 |
| 7 | 62.98 ± 5.878 | – | 412.00 ± 4.917 | – |
| 8 | >300 | – | >600 | – |
| 9 | >300 | – | >600 | – |
| 10 | >300 | – | >600 | – |
| Miltefosine | 8.56 ± 0.695 | 11.615 ± 1.790 | 152.61 ± 3.855 | 13.13 |
IC50: inhibitory concentration of 50% parasites. CC50: cytotoxicity concentration of 50% cells. SI: selectivity index calculated from the ratio of CC50 versus the IC50 for intracellular amastigotes. –: not determined. Data represent mean ± standard deviation of three experiments performed at least in triplicate.