Antileishmanial activities (μM ± standard deviation) of compounds against L. major strain IR173.
| Compd. | General cytotoxicity Vero IC50 (μM) | Host cell cytotoxicity THP-1 IC50 (μM) | Anti-promastigote activity | Anti-amastigote activity | ||||
|---|---|---|---|---|---|---|---|---|
| IC50 (μM) | SI1a | IC50 (μM) | SI2b | SI3c | SpI1d | |||
| NFA | 17.82 ± 0.25 | 80.92 ± 6.37 | 7.94 ± 0.79 | 2 | 5.60 ± 0.44 | 3 | 14 | 1.42 |
| 1a | 16.29 ± 3.50 | >100 | 1.19 ± 0.29 | 14 | >10 | — | — | — |
| 2a | 47.42 ± 1.12 | 63.37 ± 5.49 | 0.73 ± 0.09 | 65 | 3.69 ± 0.24 | 13 | 17 | 0.20 |
| 3a | >100 | >100 | 0.42 ± 0.07 | 238 | 2.47 ± 0.43 | 40 | 40 | 0.17 |
| 4a | >100 | >100 | 0.75 ± 0.18 | 133 | 0.63 ± 0.02 | 159 | 159 | 1.19 |
| 5a | >100 | >100 | 0.42 ± 0.08 | 238 | >10 | — | — | — |
| 6a | 51.01 ± 1.26 | >100 | 0.89 ± 0.12 | 57 | >10 | — | — | — |
| 7a | >100 | >100 | 0.45 ± 0.02 | 222 | >10 | — | — | — |
| 8a | 18.66 ± 1.31 | 46.20 ± 5.02 | 0.64 ± 0.10 | 29 | >10 | — | — | — |
| 9a | 11.56 ± 1.12 | 16.75 ± 1.14 | 0.70 ± 0.10 | 17 | 7.90 ± 0.19 | 1 | 2 | 0.09 |
| NTA | 12.42 ± 0.88 | 26.69 ± 0.72 | 3.75 ± 0.39 | 3 | >10 | — | — | — |
| 1b | 42.00 ± 8.79 | >100 | 1.43 ± 0.19 | 29 | >10 | — | — | — |
| 2b | >100 | >100 | 3.79 ± 0.70 | 26 | >10 | — | — | — |
| 7b | >100 | >100 | 4.39 ± 0.24 | 23 | >10 | — | — | — |
| 8b | 33.12 ± 1.22 | 22.87 ± 0.13 | 2.22 ± 0.00 | 15 | >10 | — | — | — |
| 11 | >100 | — | >10 | >10 | ||||
| 12 | >100 | — | >10 | >10 | ||||
| NFZ | >100 | >100 | 1.85 ± 0.06 | 54 | >10 | — | — | — |
| FZD | >100 | >100 | 0.34 ± 0.03 | 294 | 5.61 ± 1.89 | 18 | 18 | 0.06 |
| Em | 0.08 ± 0.009 | — | — | — | — | — | — | |
| Bzn | >100 | >100 | — | — | — | — | — | |
| AmB | 57.80 ± 3.20 | 14.86 ± 0.09 | 0.03 ± 0.01 | 1927 | 0.47 ± 0.01 | 123 | 32 | 0.06 |
a
Selectivity indexes of L. major: SI1 = IC50 Vero/IC50 promastigote.
b
SI2 = IC50 Vero/IC50 amastigote.
c
SI3 = IC50 THP-1/IC50 amastigote. Specificity index (SpI) < 0.4 indicates more antipromastigote activity, 0.4 < SpI < 2.0 indicates activity against both forms, SpI > 2.0 indicates more anti-amastigote activity.55
d
Specificity index of L. major: SpI1 = IC50 promastigote/IC50 amastigote. Selectivity Indexes of L. donovani.