Table 6.
In vitro intraerythrocytic antimalarial activity of 2 against field adapted strains (chloroquine and artesunate as controls).[a]
|
Field adapted strain |
Mutated loci |
Compound 2, IC50 [μM][b] (fold shift) |
Chloroquine IC50 [μM][b] |
Artesunate IC50 [μM][b] |
|---|---|---|---|---|
|
NF54 |
|
0.55 (−) |
0.008 |
0.004 |
|
K1 |
Pfcrt, Pfmdr1, Pfdhfr, Pfdhps |
0.62 (1.1) |
0.20 |
0.002 |
|
7G8 |
Pfcrt, Pfmdr1, Pfdhfr, Pfdhps |
0.47 (0.8) |
0.08 |
0.002 |
|
TM90 C2b |
Pfcrt, Pfmdr1, Pfdhfr, Pfdhps, PfcytbQ0 |
0.72 (1.3) |
0.14 |
0.005 |
|
Cam3.I |
Pfcrt, Pfmdr1, Pfdhfr, Pfdhps, Pfkelch13 |
0.79 (1.4) |
0.18 |
0.011 |
|
Dd2 |
Pfcrt, Pfmdr1, Pfdhfr, Pfdhps |
0.90 (1.6) |
0.16 |
0.006 |
[a] 72‐hour [3H]hypoxanthine incorporation assay. [b] mean values from two independent biological replicates.