Table 7.
In vitro intraerythrocytic antimalarial activity of 2 against laboratory selected P. falciparum resistant strains.[a]
|
Lab adapted strains (mutated loci) |
Compound 2, IC50 [μM][b] (fold shift) |
Ref. compounds, Dd2 (wt)/lab adapted strains (IC50 [nM][b] (fold shift) |
|---|---|---|
|
Dd2 (wt) |
0.895 (−) |
|
|
Dd2 (PfeEF2)9 |
1.64 (1.8) |
2/3100 (1550)[c] |
|
Dd2 (Pfpi4k)12 |
0.778 (0.9) |
21.2/102 (4.8)[d] |
|
Dd2 (Pfdhodh)13 |
0.699 (0.8) |
8.0/143 (18) [e] |
|
Dd2 (Pfcarl)5 |
0.718 (0.8) |
41/2992 (73) [f] |
|
Dd2 (Pfcytb)14 |
0.707 (0.8) |
19/254 (13) [g] |
[a] Genetically engineered P. falciparum strains. Mutations were introduced in the Dd2 wild‐type strain. [b] Values reported are means of at least two independent experiments. Reference compounds; [c] M5717. [d] MMV390048. [e] DSM265. [f] GNF153. [g] ELQ300.