Antileishmanial activities and cytotoxicity (μM ± standard deviation) of compounds against L. donovani strain 9515.
| Compd. | Anti-promastigote activity | Anti-amastigote activity | ||||
|---|---|---|---|---|---|---|
| IC50 (μM) | SI4a | IC50 (μM) | SI5b | SI6c | SpI2d | |
| NFA | >10 | — | 2.68 ± 0.68 | 2 | 30 | — |
| 1a | 1.45 ± 0.19 | 11 | >10 | — | — | — |
| 2a | 1.18 ± 0.14 | 40 | >10 | — | — | — |
| 3a | 0.67 ± 0.04 | 149 | >10 | — | — | — |
| 4a | 3.56 ± 0.00 | 28 | 6.41 ± 0.00 | 16 | 16 | 0.56 |
| 5a | 0.76 ± 0.05 | 132 | >10 | — | — | — |
| 6a | 1.16 ± 0.11 | 44 | 2.28 ± 0.07 | 22 | 44 | 0.51 |
| 7a | 1.61 ± 0.22 | 62 | 0.25 ± 0.09 | 400 | 400 | 6.44 |
| 8a | 1.02 ± 0.08 | 18 | 2.70 ± 0.62 | 7 | 17 | 0.38 |
| 9a | 0.70 ± 0.06 | 17 | 0.53 ± 0.22 | 22 | 32 | 1.32 |
| NTA | 5.07 ± 0.45 | 2 | >10 | — | — | — |
| 1b | 0.93 ± 0.06 | 45 | 7.26 ± 2.56 | 6 | 14 | 0.13 |
| 2b | 2.00 ± 0.15 | 50 | >10 | — | — | |
| 8b | 1.66 ± 0.18 | 20 | 0.34 ± 0.03 | 97 | 67 | 4.88 |
| 11 | >10 | >10 | ||||
| 12 | >10 | >10 | ||||
| NFZ | 1.85 ± 0.14 | 54 | 1.69 ± 0.36 | 59 | — | 1.09 |
| FZD | 0.28 ± 0.28 | 357 | 2.70 ± 0.81 | 37 | — | 0.10 |
| AmB | 0.02 ± 0.009 | 2890 | 0.45 ± 0.05 | 128 | — | 0.04 |
a
SI4 = IC50 Vero/IC50 promastigote.
b
SI5 = IC50 Vero/IC50 amastigote.
c
SI6 = IC50 THP-1/IC50 amastigote.
d
Specificity index of L. donovani: SpI2 = IC50 promastigote/IC50 amastigote. Selectivity indexes of T. cruzi.