In vitro cytotoxicity using macrophage J774.1A, antiamastigote activity, and the relative selectivity index of compounds 3a–h.
| ||||
|---|---|---|---|---|
| Compds (X, Y) | CC50a (μM) | S.I.b | IC50c (μM) (S.I.) | |
| Macrophage | Promastigote | Epimastigote | Axenic amastigote | |
| J774.1a | L. infantum | T. cruzi | L. infantum | |
| 3a (H, NO2) | 15.06 ± 0.11 | 17.1 | 23.9 | 0.93 ± 0.04 (16.2) |
| 3b (4-F, NO2) | 69.06 ± 3.99 | 15.1 | 16.8 | 3.52 ± 0.35 (19.6) |
| 3f (3-Cl, NO2) | 41.55 ± 1.87 | 54.0 | 60.2 | 0.89 ± 0.03 (46.7) |
| 3h (4-F, H) | 119.15 ± 8.12 | 13.1 | 5.7 | 11.12 (10.7) |
| Miltefosined | 89.21 ± 7.01 | 8.9 | — | 8.69 ± 0.03 (10.1) |
| Nifurtimoxe | 280.00 ± 4.00f | — | 36.3 | — |
a
The results are the mean of three independent experiments.
b
S.I.: selectivity index calculated as CC50/IC50 (promastigote or epimastigote).
c
Selectivity index was calculated as CC50/IC50 (axenic amastigote).
d
Miltefosine as antileishmanial reference drug (from ref. 25).
e
Nifurtimox as antichagasic reference drug.
f
From ref. 45.