Table 4.
Antimalarial activity of APAQs in asynchronous blood culture
| Compound | Pred. PfDHODH | XC50 (µM)a,b | Resistance ratio (±) | |
|---|---|---|---|---|
| Ki (µM) | 3d7(−) | Dd2(+) | ||
| 12a | 0.049 | 10.0 | 46 | 4.6 |
| 12b | 0.051 | 1.61 | 6.4 | 3.9 |
| 11a | 0.023 | 0.55 | 2.3 | 4.1 |
| 11c | 0.037 | 0.37 | 1.78 | 4.8 |
| 8 | 0.037 | 0.30 | 1.47 | 5.0 |
| 9 | 0.025 | 0.106 | 0.21 | 2.0 |
| 11b | 0.038 | 0.037 | 0.24 | 6.6 |
| CID 44534046c | 0.112 | 0.89 | 4.6 | 5.2 |
| CID 44535189c | 0.077 | 0.85 | 8.6 | 10.1 |
PfDHODH dihydroorotate dehydrogenase from Plasmodium falciparum, Ki inhibition constant, Pred predicted
aConcentration required to reduce parasite growth rate by 50%
b(−) and (+) denote chloroquine-susceptible and -resistant strains, respectively
cMost active APAQs in the GSK data set