TABLE 2.
Leishmanicidal activities for different forms of L. infantum and cytotoxicities of quinolin-4(1H)-imine derivatives
| Compound | Mean value ± SD fora: |
SIb | |||
|---|---|---|---|---|---|
| IC50 (μM) against: |
CC50 (μM) in BMDM | ||||
| Promastigotes | Axenic amastigotes | Intramacrophagic amastigotes | |||
| 1d | 2.8 ± 0.6 | 19.4 ± 1.4 | 1.3 ± 0.5 | 10.1 ± 3.4 | 7.8 |
| 1e | ND | 11.3 ± 1.1 | 2.2 ± 0.6 | 14.4 ± 1.9 | 6.5 |
| 1f | 4.5 ± 0.3 | 12.2 ± 1.9 | 1.7 ± 0.4 | 10.8 ± 0.9 | 6.4 |
| 1g | 2.3 ± 0.2 | 11.4 ± 0.8 | 1.4 ± 0.6 | 9.6 ± 0.9 | 6.9 |
| 1h | 1.5 ± 0.3 | 10.9 ± 0.5 | 0.9 ± 0.1 | 10.0 ± 1.8 | 11.1 |
| 1i | 1.4 ± 0.1 | 5.8 ± 2.8 | 1.1 ± 0.3 | 9.1 ± 1.4 | 8.3 |
| 1j | 1.9 ± 0.1 | 14.1 ± 4.2 | 1.4 ± 0.3 | 9.5 ± 1.0 | 6.8 |
| 1k | 2.50 ± 0.01 | 11.0 ± 1.7 | 1.9 ± 0.5 | 10.9 ± 1.5 | 5.7 |
| 1l | 2.42 ± 0.02 | 15.8 ± 2.3 | 1.9 ± 0.2 | 10.8 ± 1.0 | 5.7 |
| 1m | 1.7 ± 0.2 | 13.4 ± 3.0 | 1.3 ± 0.2 | 8.4 ± 2.1 | 6.5 |
| 1n | 1.9 ± 0.2 | 6.5 ± 2.8 | 0.7 ± 0.2 | 6.8 ± 0.8 | 9.7 |
| 2c | ND | ND | >0.5 | <0.5 | |
| AMBc | 0.17 ± 0.09 | 0.39 ± 0.24 | 0.06 ± 0.01 | 3.1 ± 0.6 | 52 |
a
L. infantum promastigotes, axenic amastigotes, and intramacrophagic amastigotes, as well as BALB/c mouse BMDM, were incubated for 24 h with different concentrations of the different compounds. IC50, half-maximal inhibitory concentration; CC50, 50% cytotoxic concentration; ND, not determined.
b
SI, selectivity index (ratio between CC50 and IC50 values for intramacrophagic amastigotes).
c
AMB, amphotericin B, used as a positive control.