Table 3.
In vitro activities of 23–32 against P. falciparum strains (3D7, W2, FCR3 and BreI) with respect to CQ and FQ. Activities of 23–32 are in μM units whereas those of CQ and FQ are in nM units.
| Compounds | Plasmodium strains (IC50 values) |
|||
|---|---|---|---|---|
| 3D7 | W2 | FCR3 | BReI | |
| 23 | 30.2 ± 6.1 | 95.8 ± 20.4 | 74.0 ± 15.4 | 46.0 ± 14.4 |
| 24 | 33.0 ± 6.4 | 28.3 ± 9.9 | 31.2 ± 5.8 | 34.0 ± 8.1 |
| 25 | 0.2 ± 0.1 | 0.8 ± 0.2 | 0.2 ± 0.1 | 1.0 ± 0.4 |
| 26 | 0.3 ± 0.2 | 0.3 ± 0.1 | 0.6 ± 0.1 | 0.3 ± 0.1 |
| 27 | 0.1 ± 0.0 | 0.2 ± 0.1 | 0.8 ± 0.2 | 0.6 ± 0.2 |
| 28 | 64.2 ± 12.8 | 68.2 ± 10.6 | 30.2 ± 5.6 | 33.0 ± 8.5 |
| 29 | 20.7 ± 6.3 | 21.8 ± 7.9 | 22.2 ± 5.9 | 17.0 ± 3.5 |
| 30 | 0.2 ± 0.1 | 0.2 ± 0.1 | 0.8 ± 0.2 | 0.8 ± 0.2 |
| 31 | 0.3 ± 0.1 | 0.3 ± 0.1 | 0.5 ± 0.1 | 0.4 ± 0.1 |
| 32 | 0.6 ± 0.1 | 2.0 ± 0.4 | 0.5 ± 0.2 | 0.7 ± 0.1 |
| CQ | 23.9 ± 4.6 | 540.0 ± 87.5 | 645.0 ± 63.1 | 396.2 ± 54.2 |
| FQ | 3.5 ± 0.5 | 7.1 ± 1.8 | 1.8 ± 0.3 | 3.0 ± 1.0 |