Table 1. In vitro screening data against three different trypanosomatids.
ID No | T.b.rhod.a | SI | T. cruzib | SI | L.don. axen.c | SI | Cytotox. L6 | Bnz/Comp. | Chemical Structure |
---|---|---|---|---|---|---|---|---|---|
IC-50 μM | IC-50 μM | IC-50 μM | IC-50 μM | ||||||
1 | 1.38 | >14 | 0.34 | >562 | 58.15 | >3 | >191.1 | 4.6 | |
2 | 1.2 | 99 | 0.412 | 287 | 44.45 | 3 | 118.4 | 3.8 | |
3 | 5.33 | 10 | 0.04 | 1320 | 25.92 | 2 | 52.79 | 39.2 | |
4 | 49.6 | 5.2 | 1.678 | 152 | >100 | 1 | >100 | 0.9 | |
5 | 35.65 | 4.3 | 0.848 | 180 | >315 | <1 | 152.68 | 1.9 | |
6 | 1.34 | 114.6 | 8.8 | 17.5 | >315 | <1 | 153.9 | 0.2 | |
7 | 0.231 | 180.2 | 0.048 | 868 | 11.35 | 3.7 | 41.7 | 32.7 | |
8 | 23.85 | 5.1 | 0.419 | 289 | 173.45 | <1 | 121.34 | 3.7 | |
9 | 35.56 | 3.5 | 0.556 | 224.5 | >238.66 | <1 | 124.8 | 2.8 | |
10 | 10.46 | 10.8 | 0.828 | 137 | 180.2 | <1 | 113.3 | 2.5 | |
11 | 0.78 | 42.9 | 0.286 | 117 | 23.9 | 1.4 | 33.5 | 7.1 | |
12 | 15.62 | 13 | 4.7 | 43.1 | >290 | <1 | 202.9 | 0.3 | |
13 | 62.4 | 2.2 | 34.4 | 4 | 186.4 | <1 | 137.1 | 0.1 | |
14 | 10.74 | 7.4 | 9.4 | 8.4 | 149.5 | <1 | 79.2 | 0.2 | |
15 | 0.204 | 500 | 0.059 | 1725 | 4.49 | 22.7 | 101.9 | 26.6 | |
16 | 0.954 | 170 | 0.566 | 287 | 20 | 8.1 | 162.5 | 3.6 | |
17 | 0.355 | 125.6 | 0.142 | 314 | 4.1 | 10.9 | 44.54 | 14.4 | |
18 | 7.61 | 6.5 | 3.23 | 15.3 | 4.27 | 11.6 | 49.5 | 0.6 | |
19 | 52.5 | 3.4 | 4.88 | 36.1 | 11.4 | 15.4 | 176 | 0.4 | |
20 | 3.87 | 11.1 | 1.75 | 24.6 | 7.3 | 5.5 | 43 | 1.2 |
STIB 900 trypomastigotes;
Tulahuen C4 amastigotes;
MHOM-ET-67/L82 amastigotes; Cytotoxicity was measured in L6 cells. SI = IC50 in L6 cells / IC50 in each type of parasites. The reference compounds were: Melarsoprol (T. b. rhodesiense; IC50 = 0.011 0.004), Benznidazole (Bnz; T. cruzi; IC50 = 1.85 0.33) and Miltefosine (L. donovani; IC50 = 0.378 0.011). Bnz/comp.: The ratio of IC50 values of Benznidazole and each tested compound against T. cruzi. The IC50 values are the means of two independent assays and varies less than ± 50%. Green color indicates active compounds, light red, moderately active, light blue, toxic and no color, inactive. Compounds 1-3 have been described before [10].