Table 2. In Vitro Activities against Intramacrophage L. infantum Amastigotes.
| compd | in vitro antiamastigote activity at 0.5 μMa | in vitro antiamastigote activity IC50 (μM)b | THP-1 IC50 (μM)c | SI (THP/IPT)d |
|---|---|---|---|---|
| 8 | 29.6 | 1.91 | 3.29 | 1.72 |
| 10 | 72.2 | 0.31 | 1.00 | 3.22 |
| 11 | 26.4 | 1.85 | 2.96 | 1.60 |
| 13 | 38.9 | 1.29 | 4.25 | 3.29 |
| 14 | 26.4 | >1 | 1.91 | <1.91 |
| 15 | 47.6 | 0.58 | 4.73 | 8.15 |
| 18 | 42.7 | 0.65 | 2.35 | 3.61 |
| 19 | 36.9 | 0.73 | 2.44 | 3.34 |
| 20 | 42.2 | 0.79 | 2.79 | 3.51 |
| 24 | 29.6 | >1 | 2.31 | <2.31 |
| controle | 95.5 | 0.21 | >10.8 | >51.4 |
Mean value of two or three experiments.
Mean value of two experiments.
Cytotoxicity against differentiated THP-1, human monocytic cell line derived from an acute monocytic leukemia patient.
Selectivity index (IC50 against THP-1/IC50 against intracellular amastigotes).
Control drug: amphotericin B.