Table 1.
IC50 values of compounds 1–3 and 1A–3A against Trypanosoma brucei pteridine reductase 1 (TbPTR1) and Leishmania major pteridine reductase 1 (LmPTR1). Standard deviations agreed to ±10%. NI: No Inhibition. The percentage of inhibition at 50 μM is reported in Table S1 of the Supporting Information. The control compound was pyrimethamine, a PTR1 inhibitor (100% inhibition at 50 μM against both PTR1 enzymes). NI = No Inhibition (percentage of inhibition lower than 15%).
| Compound | IC50 TbPTR1 (μM) | IC50 LmPTR1 (μM) |
|---|---|---|
| 1 | 31.0 | 57.0 |
| 2 | 133.0 | 35.0 |
| 3 | 82.0 | 36.0 |
| 1A | 4.3 | 12.5 |
| 2A | NI at 50 μM | NI at 50 μM |
| 3A | 38.0 | 35.0 |