Table 2. IC50 Leishmanicidal and Cytotoxic Effects from 2-Acylpyrrole Series 5a and 5b (Expressed as μM) on In Vitro Promastigote Assays.
|
L. amazonensis |
L. donovani |
macrophages J774 | ||||
|---|---|---|---|---|---|---|
| entry | comp. | IC50 ± SD (μM)a | SIb | IC50 ± SD (μM)a | SIb | CC50 ± SD (μM)c |
| 1 | 5aa | 259.58 ± 40.72 | >1.55 | N/Ad | 401.17e | |
| 2 | 5ab | N/Ad | N/Ad | 381.24e | ||
| 3 | 5ac | 32.88 ± 0.74 | >2.77 | 58.54 ± 7.04 | >1.55 | 91.02 ± 6.55 |
| 4 | 5ad | N/Ad | N/Ad | 270.19 ± 26.30 | ||
| 5 | 5ae | 117.09 ± 10.92 | >3.01 | 189.77 ± 6.76 | >1.86 | 352,46e |
| 6 | 5af | 67.18 ± 4.94 | >4.54 | 118.18 ± 25.81 | >2.58 | 304.72e |
| 7 | 5ag | N/Ad | N/Ad | 364.59e | ||
| 8 | 5ah | N/Ad | N/Ad | 339.82e | ||
| 9 | 5ai | 48.02 ± 1.61 | >3.13 | 42.82 ± 0.61 | >3.51 | 150.36 ± 49.40e |
| 10 | 5aj | 32.55 ± 0.64 | >2.71 | 210.90 ± 32.77 | >0.42 | 88.29 ± 3.36e |
| 11 | 5ak | N/Ad | N/Ad | 87.27 ± 7.37e | ||
| 12 | 5al | N/Ad | N/Ad | 224.28 ± 46.89e | ||
| 13 | 5am | 57.34 ± 0.25 | >4.53 | 198.54 ± 25.36 | >1.31 | 259.56e |
| 14 | 5an | 36.11 ± 1.23 | >3.12 | 58.50 ± 3.34 | >1.93 | 112.82 ± 39.19e |
| 15 | 5ba | 152.77 ± 21.65 | >2.50 | N/Ad | 381.23e | |
| 16 | 5bb | 149.20 ± 3.84 | >2.43 | 119.64 ± 14.98 | >3.02 | 361.87e |
| 17 | 5bc | 30.87 ± 3.11 | >10.17 | 221.31 ± 36.90 | >1.42 | 314.05e |
| 18 | 5bd | 16.87 ± 0.73 | >10.67 | 7.78 ± 0.27 | >23.15 | 136.96 ± 36.42 |
| 19 | 5be | 51.46 ± 4.72 | >2.89 | 20.69 ± 0.98 | >7.19 | 148.74 ± 19.33 |
| 20 | 5bf | 38.10 ± 0.85 | >3.14 | 19.87 ± 1.47 | >6.01 | 119.51 ± 37.36e |
| 21 | 5bg | 191.77 ± 12.04 | >1.81 | 315.43 ± 60.80 | >1.10 | 348.04e |
| 22 | 5bj | 71.06 ± 7.81 | >1.53 | 43.51 ± 0.59 | >0.80 | 108.45 ± 5.76e |
| 23 | 5bk | N/Ad | N/Ad | 283.78 | ||
| 24 | 5bo | 224.26 ± 14.71 | >1.53 | 172.92 ± 60.34 | >1.98 | 342.07e |
| 25 | 5bp | 207.96 ± 23.62 | >1.31 | 184.22 ± 8.67 | >1.47 | 356.76e |
| 26 | 5bq | 209.16 ± 4.69 | >1.56 | 92.81 ± 7.68 | >1.08 | 325.31e |
| 27 | 5br | 226.54 ± 13.42 | >1.66 | N/Ad | 376.90e | |
| 28 | 5bs | N/Ad | N/Ad | 396.40e | ||
| 29 | miltefosine | 30.67 ± 8.80 | 1.80 | 0.24 ± 0.02 | 230.83 | 55.40 ± 4.19 |
a
IC50: concentration of the compound that produced a 50% reduction in parasites; SD: standard deviation.
b
SI: selectivity index, SI = CC50/IC50.
c
CC50: concentration of the compound that produced a 50% reduction of cell viability in treated culture cells with respect to untreated ones.
d
N/A: not active at the maximum dose tested (100 μg/mL).
e
CC50 values, expressed as μM, correspond to 100 μg/mL, which was the higher doses tested.