Table 3.
Cruzain inhibition and trypanocidal activity of compounds with modifications to the aromatic ring.
 | |||
|---|---|---|---|
| Compound | Structure | IC50 cruzain (μM)a | IC50 T. cruzi (μM)b |
| 3k |  |
ND | 3.9 ± 0.9 |
| 3k' |  |
75.0 ± 1.0 | >100 |
| 3l |  |
ND | >100 |
| 3l' |  |
75.5 ± 2.5 | >100 |
| 3m' |  |
32.8 ± 8.0 | >100 |
| 3d |  |
16.7 ± 1.3 | >100 |
| 3e |  |
20.5 ± 1.3 | >100 |
| 3i |  |
2.1 ± 1.3 | 32.8 ± 4.9 |
a
IC50 values against cruzain were independently determined by obtaining rate measurements in triplicate for at least six inhibitor concentrations. The values represent the mean ± SD of three individual experiments.
b
IC50 values against T. cruzi represent the mean ± SD of two individual experiments. ND, not determined.