Table 2. Cytotoxicity, Leishmania Antiamastigote Activity, and Selectivity Indexes of Active Derivatives 3a–f.
| compounds | peritoneal macrophage, CC50 (μM) | J774.1A macrophage, CC50 (μM) | amastigote, IC50 (μM) L. braziliensis (S.I.Leishmania)a | epimastigote, IC50 (μM) T. cruzi (S.I.T.cruzi)b | |
|---|---|---|---|---|---|
| 1 | 3a | 61.02 ± 2.34 | 90.20 ± 4.32 | 8.26 ± 0.45 (7.4) | <3.6 |
| 2 | 3b | >100.0 | >120.00 | 7.41 ± 0.39 (>13.5) | >6.7 |
| 3 | 3c | 89.86 ± 3.77 | 104.78 ± 5.66 | 8.96 ± 0.53 (10.0) | 9.1 |
| 4 | 3d | 77.98 ± 3.89 | 78.59 ± 3.99 | 12.67 ± 0.78 (6.2) | 5.5 |
| 5 | 3e | 84.76 ± 3.67 | 114.58 ± 5.43 | 13.99 ± 0.89 (6.1) | 6.4 |
| 6 | 3f | >100.0 | >120.0 | 8.43 ± 0.51 (>11.9) | no active |
| 7 | miltefosine | 67.78 ± 3.11 | 72.34 ± 3.45 | 21.23 ± 1.13 (3.2) | |
| 8 | glucantime | 138.22 ± 10.11 | 12.21 ± 2.12 (11.3) | ||
| 9 | nifurtimox | 280.0 ± 4.00c | 36c |
a
Selectivity indexes calculated from ratio between the CC50 (peritoneal macrophage) and IC50 (amastigotes of L. braziliensis).
b
Selectivity indexes calculated from the ratio between the CC50 (J774.1A) and IC50 of epimastigotes (T. cruzi).
c
From ref (36).