Table 16.
Antitrypanosomal activity and SI of compounds 21b-f against T. cruzi and T. brucei.
| |||||
|---|---|---|---|---|---|
| Compound | R |
T. cruzi
IC50a |
SIb |
T.b. brucei
IC50 |
SIc |
| 21b | 5-Cl | 0.5 | 15.9 | 4.4 | 84% |
| 21c | 5-Br | 0.79 | >63.3 | 16 | >5.18 |
| 21d | 6-Cl | 0.5 | 12.6 | 2.4 | >34.6 |
| 21e | 6-Br | 0.4 | 32.5 | 1.5 | >55.3 |
| 21f | 6-F | 1.3 | 19.2 | 0.90 | 15.5 |
| Benznidazole | 1.58 | 20 | nd | nd | |
| Pentamidine | nd | nd | 0.0014 | nd | |
Note: aIC50: compound concentration that reduced the parasite load of 50%; bSI: selectivity index (CC50 H9c2 /IC50 T. cruzi); cSI: selectivity index (CC50 HEK-293 /IC50 T. brucei); nd = not determined.