Table 2.
Compound | a UM01 (macaque RBC) EC50 (nM) (range/2) | b A1-H.1 (human RBC) EC50 (nM) ± SEM | Fold difference (A1-H.1/UM01) |
---|---|---|---|
Endoperoxides | |||
Dihydroartemisinin | 2.1 (0.4) | 2.0 ± 0.3 | 0.95 |
Artesunate | 13.8 (3.6) | 10.9 ± 1.7 | 0.79 |
Artefenomel (OZ439) | 4.4 (1.6) | 6.6 ± 1.4 | 1.5 |
Quinolines and amino-alcohols | |||
Chloroquine | 21.5 (4.9) | 29.3 ± 4.7 | 1.36 |
Mefloquine | 13.1 (2.5) | 10.9 ± 1.7 | 0.83 |
Quinine | 40.3 (0.4) | 54.8 ± 3.0 | 1.36 |
Ferroquine | 9.8 (2.32) | 12.2 ± 1.6 | 1.24 |
Dihydrofolate reductase inhibitors | |||
Pyrimethamine | 3.2 (0.5) | 5.1 ± 0.8 | 1.59 |
Cycloguanil | 0.7 (0.1) | 1.3 ± 0.3 | 1.86 |
Trimethoprim | 137 (54) | 265 ± 47 | 1.93 |
P218 | 0.68 (0.04) | 4.1 ± 0.7 | 6.03 |
Other | |||
Atovaquone | 4.1 (0.04) | 2.6 ± 0.4 | 0.63 |
Pyronaridine | 4.9 (0.84) | 10.7 ± 1.6 | 2.18 |
DSM265 | 170 (66) | 303 ± 15 | 1.78 |
DSM421 | 142 (71) | 194 ± 23 | 1.37 |
Cipargamin (KAE609) | 3.8 (1.6) | 6.1 ± 0.5 | 1.61 |
PA21A092 | 35.7 (2.8) | 63.8 ± 7.6 | 1.79 |
AN13762 | 3618 (110) | 2762 ± 296 | 0.76 |
Parasites were exposed to the compounds for a single life cycle (27 h).
UM01 data are the mean of two independent experiments each performed in duplicate. The range/2, calculated for the two experiments, is shown in parentheses.
Data reported previously (van Schalkwyk et al., 2017) or from Table 1 above. Data are the mean ± SEM for at least three experiments each performed in duplicate.