Table 1. Compound structures and activity against purified T. cruzi PFT, T. cruzi cells, and murine fibroblast cells.
Compound | R1 | R2 | % inhibition of T. cruzi PFT at 50 nM of drug | ED50 against T. cruzi,* μM | ED50 against murine 3T3 fibroblasts, μM |
---|---|---|---|---|---|
1 | CO2CH3 | Phenyl | 0.8 | 0.0005 | >10 |
2 | CO2CH3 | H | 4 | 0.08 | >10 |
3 | H | Phenyl | 10 | 0.01 | 10 |
4 | Phenyl | 23 | 0.05 | >10 | |
5 | Phenyl | 16 | 0.02 | >10 |
R groups in reference to Fig. 1c.
Mammalian-stage parasites grown in 3T3 fibroblasts