Table 3.
Anti-Mtb, anti-HIV-1, anti-malarial, and anti-leishmania data
| Compound | Mycobacterium tuberculosis (H37Rv) MIC (μg/mL) | P. falciparum (D6 clone) IC50 (μg/mL) | P. falciparum (chloroquine-resistant W2 clone) IC50 (μg/mL) | Cytotoxicity (Vero) TC50 (μg/ml) | Anti-HIV-1
|
Leishmania donovani
|
||
|---|---|---|---|---|---|---|---|---|
| EC50 (μM) | EC90 (μM) | IC50 (μg/mL) | IC90 (μg/mL) | |||||
| 2 | — | 1.1 | 0.4 | — | 0.6 | — | 0.7 | 1.1 |
| 3 | >128 | 2.0 | 1.3 | NC | 1.3 | 8.0 | 1.7 | 2.7 |
| 4 | >128 | 0.3 | 1.1 | NC | 0.5 | 3.0 | 0.1 | 0.2 |
| 5 | >128 | 0.4 | 1.5 | NC | 10.9 | 33.5 | 1.3 | 2.5 |
| 6 | >128 | 1.8 | 3.8 | NC | 37.7 | 70.6 | 4.1 | 9.5 |
| 7 | >128 | 1.8 | 4.1 | NC | 2.1 | 10.5 | 1.4 | 2.5 |
| 8 | >128 | 2.9 | NA | NC | 45.9 | 95.4 | 6.8 | 12.0 |
| 9 | >128 | 3.3 | 3.7 | NC | 4.6 | 33.9 | 1.7 | 2.7 |
| 10 | >128 | 0.6 | 0.9 | NC | 4.0 | 25.2 | 1.6 | 2.7 |
| 11 | >128 | 0.4 | 0.8 | NC | 9.9 | 30.6 | 1.8 | 5.5 |
| 12 | >128 | 0.6 | 2.5 | NC | 2.3 | 16.3 | 1.8 | 5.0 |
| 13 | >128 | 0.3 | 1.2 | NC | 3.8 | 7.1 | 1.5 | 2.5 |
| 14 | >128 | 0.4 | 1.3 | NC | 18.8 | 66.4 | 1.4 | 2.6 |
| 15 | >128 | 0.4 | 1.1 | NC | 16.6 | 54.3 | 6.0 | 11.0 |
| 16 | >128 | 0.2 | 1.0 | NC | 9.2 | 29.1 | 1.6 | 2.6 |
| 17 | >128 | 0.2 | 1.0 | NC | 3.7 | 6.9 | 0.4 | 0.7 |
| 18 | >128 | 3.0 | NA | NC | >100 | >100 | 26.0 | 42.0 |
| 19 | >128 | 3.0 | 4.3 | NC | 52.8 | >100 | 6.2 | 12.0 |
| 20 | >128 | 0.8 | 1.5 | NC | 8.2 | 25.3 | 4.8 | 10.0 |
| 21 | 41.03 | 0.3 | 0.8 | NC | 33.7 | 60.1 | 4.3 | 9.5 |
| Pentamidine | — | — | — | — | — | — | 1.6 | 3.5 |
| Amphotericin B | — | — | — | — | — | — | 1.1 | 2.3 |
| Chlorquine | — | 0.0165 | 0.140 | — | — | — | — | — |
IC50 and IC90 are the sample concentrations that kill 50% and 90% cells compared to the solvent controls. For malarial assays, screens were run at 4760, 1587, and 528.8 ng/mL. For Leishmania assays, screens were run at 50, 12.5, and 3.125 μg/mL NA, not active; NT, not tested: NC, not cytotoxic (4.7 μg/mL).