Table 1.
Compound | Structure | IC50 cruzain (μM)a | IC50 T. cruzi (μM)b |
Initial hit (3a) | 2.2 ± 0.4 | >100 | |
10b | 4.2 ± 1.5 | >100 | |
10c | 2.3 ± 1.0 | 0.9 ± 0.3 | |
10d | 12.0 ± 1.0 | 18.5 ± 3.1 | |
10e | 2.5 ± 0.6 | 1.2 ± 0.3 | |
10f | 0.6 ± 0.1 | 2.0 ± 0.7 | |
10k | ND | >100 | |
10l | ND | 11.6 ± 2.4 | |
10m | ND | 1.8 ± 0.4 | |
10n | ND | 1.6 ± 0.5 | |
10o | ND | 1.7 ± 0.5 | |
BZ | - | ND | 3.0 ± 0.6 |
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.
IC50 values against T. cruzi represent the mean ± SD of two individual experiments. ND, not determined.