TABLE 1.
Antimalarial and antileishmanial activities of compounds 1 to 10
| Compound | Compounda | IC50 (μg/ml) for P. falciparumb:
|
IC (μg/ml) for L. donovani
|
Cytotoxicity (μg/ml) | ||
|---|---|---|---|---|---|---|
| D6 (CQS) | W2 (CQR) | IC50 | IC90 | |||
| 1 | 1 | >4.8 (46) | >4.8 (45) | 2.4 | 11.3 | NCc |
| 2 | 2 | >4.7 (19) | >4.7 (34) | 1.7 | 5.4 | NC |
| 3 | 5 | >4.7 (35) | >4.7 (49) | 1.6 | 5.1 | NC |
| 4 | 7 | 3.8 | 3.5 | 2.4 | 14.3 | NC |
| 5 | 27 | NAd | NA | NA | NA | NC |
| 6 | 29 | NA | NA | NA | NA | NC |
| 7 | 8 | 1.2 | 4 | 16 | >50 | NC |
| 8 | 25 | NA | NA | NA | NA | NC |
| 9 | 26 | NA | NA | 8.3 | 32 | NC |
| 10 | 28 | NA | NA | 6.8 | >50 | NC |
| SAHA | 0.25 | 0.47 | 22 | 50 | 1.2 | |
| TSA | 0.036 | 0.043 | 0.89 | 25 | 0.095 | |
| Pentamidine | NTe | NT | 1.25 | 4.1 | NC | |
| Chloroquine | 0.014 | 0.18 | NT | NT | NC | |
a
From reference 7.
b
Numbers in parentheses represent percentages of inhibition at the tested dose.
c
NC, not cytotoxic at concentrations of up to 23.8 μg/ml.
d
NA, not active at the maximum dose tested (4.8 μg/ml in the case of the antimalarial assays and 50 μg/ml in the case of the antileishmanial assays).
e
NT, not tested.