Table 2. In vitro antiprotozoal activity (IC50, μM) in L. infantum and L. amazonensis, cytotoxicity (CC50, μM) on J774A.1 macrophages, and selectivity index (CC50/IC50).
| Comp. | IC50a (μM) | IC50a (μM) | CC50a (μM) | SIb (CC50/IC50) | SIb (CC50/IC50) | clog P |
|---|---|---|---|---|---|---|
| Promastigotes | Promastigotes | MΦJ774A.1 | L. infantum | L. amazonensis | ||
| L. infantum | L. amazonensis | |||||
| 4·H2SO4 | >100 | >100 | 348.88 ± 63.87 | d | d | — |
| 4, HCQ | >100 | >100 | 409.69 ± 24.19 | d | d | 4.12 |
| 5, HCQAA | >100 | >100 | 417.37 ± 30.95 | d | d | 4.63 |
| 7a | 36.11 ± 5.28 | 33.34 ± 1.15 | 355.22 ± 47.79 | 9.83 | 10.65 | 6.79 |
| 7b | 78.38 ± 1.60 | 72.24 ± 6.40 | 399.41 ± 55.36 | 5.10 | 5.53c | 6.64 |
| 7c | 92.82 ± 12.05 | >100 | 396.16 ± 29.49 | 4.27 | d | 6.81 |
| 7d | 93.31 ± 1.90 | >100 | 401.80 ± 28.58 | 4.31 | d | 6.56 |
| 7e | >100 | >100 | 191.04 ± 30.49 | d | d | 6.30 |
| 7f | 37.01 ± 0.27 | >100 | 206.28 ± 20.53 | 5.57 | d | 6.79 |
| 7g | 40.34 ± 5.13 | 56.42 ± 4.02 | 419.97 ± 26.88 | 10.41 | 8.17c | 7.36 |
| 7h | 28.67 ± 2.63 | 23.63 ± 1.60 | 259.43 ± 67.82 | 9.04 | 10.97c | 7.36 |
| 7i | 38.25 ± 5.89 | 36.65 ± 5.08 | 297.36 ± 36.29 | 7.77 | 8.11c | 7.36 |
| 7j | >100 | 44.11 ± 3.73 | 254.29 ± 51.50 | d | 5.77 | 6.39 |
| 7k | 81.07 ± 5.65 | 26.50 ± 1.31 | <10 | d | d | 6.39 |
| 7l | 74.50 ± 5.84 | 65.34 ± 11.72 | <10 | d | d | 6.39 |
| 7m | 50.11 ± 7.21 | 38.76 ± 5.30 | 230.06 ± 12.58 | 4.59 | 5.94c | 7.25 |
| 7n | >100 | >100 | 81.60 ± 7.69 | d | d | 5.82 |
| 7o | >100 | >100 | 238.45 ± 10.58 | d | d | 6.29 |
| AmpB | 1.05 ± 0.11 | 9.89 ± 4.09 | 92.70 ± 10.27 | 88.29 | 9.37 | — |
a
IC50 and CC50 values were calculated based on the average from triplicate of each point.
b
SI: selectivity index (CC50/IC50).
c
Treatments compared with the AmpB (amphotericin B) standard using the one-tailed t-test.
d
Does not show antiparasitic activity against the tested strain.