Table 3.
Activity of compounds 15–26 against P. falciparum 3D7 strain.[a]
|
| ||||||||
|---|---|---|---|---|---|---|---|---|
|
Cpd |
X |
Y |
Z |
Q |
R1 |
R2 |
R3 |
3D7 IC50 [μM] |
|
15 |
C |
C |
C |
N |
H |
H |
H |
4.4±0.59 |
|
16 |
C |
C |
C |
C |
OCH3 |
H |
H |
1.2±1.2 |
|
17 |
C |
C |
C |
C |
H |
H |
Cl |
0.6±0.09 |
|
18 |
O |
C |
C |
C |
H |
H |
H |
6.8±0.75 |
|
19 |
C |
C |
C |
C |
H |
CN |
H |
>10 |
|
20 |
C |
C |
C |
C |
H |
Cl |
H |
>25 |
|
21 |
C |
C |
C |
C |
H |
OCH3 |
H |
>25 |
|
22 |
C |
C |
C |
C |
CN |
H |
H |
>25 |
|
23 |
C |
C |
C |
C |
Cl |
H |
H |
>25 |
|
24 |
C |
N |
C |
C |
H |
H |
– |
10.2±0.75 |
|
25 |
C |
C |
N |
C |
H |
– |
H |
10.8±0.65 |
|
26 |
C |
C |
C |
C |
H |
H |
OCH3 |
>10.0 |
[a] Values reported are geometric mean ± SEM of at least two independent experiments.