Table 2. Anti-T. cruzi Activity and Mammalian Cytotoxicity of Synthetic Analogues with a Variation of S1 Substitutiona.
| IC50 (μM) ± SDb |
||||||
|---|---|---|---|---|---|---|
| entry | compound | S1 | trypomastigote | amastigote | CC50 (μM) ± SDc | SId |
| 1 | 1e | OH | 38.6 ± 8.3 | 86.5 ± 16.2 | >200 | >2.3 |
| 2 | 2e | OMe | NA | NA | >200 | ND |
| 3 | 5 | OMOM | 6.5 ± 4.9 | 24.4 ± 10.3 | >200 | >8.2 |
| 4 | 6 | OPMB | NA | 4.0 ± 1.4 | >200 | >50 |
| 5 | 7f | OAllyl | NA | NA | >200 | ND |
| 6 | 8f | OBn | NA | 9.5 ± 1.3 | >200 | >21.1 |
| 7 | 25 | H | NA | 10.9 ± 6.5 | >200 | >18.3 |
| 8 | benznidazole | 17.7 ± 1.9 | 5.0 ± 1.5 | 190.6 ± 13.4 | 38.1 | |
