Table 1.
Activity data for anti-malarial drugs
| COMPOUND |
3D7
a
|
NF54-pfs16-GFP
a
|
NF54-pfs16-GFP
b
|
(I-III)/ABS | (IV-V)/ABS |
|---|---|---|---|---|---|
| ABS | early (I-III) gam | late (IV-V) gam | |||
|
4-Aminoquinolines | |||||
| Amodiaquine |
255 (65) |
242 (110) |
87% |
0.9 |
|
| Naphthoquines |
411 (82) |
483 (330) |
NA |
1.2 |
|
| AQ-13 |
183 (0.01) |
453 (230) |
82% |
2.5 |
|
| Piperaquines |
1880 (210) |
3990 (2800) |
43% |
1.6 |
|
| Hydroxychloroquines |
966 (130) |
1340 (140) |
45% |
1.4 |
|
| Pyronaridine |
299 (69) |
250 (96) |
4260 (240) |
0.8 |
14.2 |
|
8-Aminoquinolines | |||||
| Pamaquine |
88% |
79% |
NA |
|
|
| Primaquine |
7120 (1500) |
NA |
74% |
|
|
| Tafenoquine |
5650 (1600) |
4800 (1500) |
4620 (1600) |
0.8 |
0.8 |
| NPC-1161B |
3360 (860) |
2180* |
4850 (2700) |
0.6 |
1.4 |
|
Endoperoxides | |||||
| Artemether |
25.8 (11) |
11 (2.8) |
3.13 (0.7) |
0.4 |
0.1 |
| Artenimol (DHA) |
2.08 (0.6) |
18.3 (17) |
2.17 (1.2) |
8.8 |
1.0 |
| Artesunate |
6.7 (1.6) |
3.8 (0.28) |
2.53 (1.10) |
0.6 |
0.4 |
| Artemisinin |
41.6 (12) |
12.1 (14) |
5.47 (2.0) |
0.3 |
0.1 |
| Artemisone |
3.72 (0.14) |
2.4 (0.85) |
1.7 (0.46) |
0.6 |
0.5 |
|
Anti folates | |||||
| Pyrimethamine |
21.5 (0.07) |
NA |
NA |
|
|
| Chlorproguanil |
6250 (520) |
108% |
4340 (840) |
|
0.7 |
| Proguanil HCl |
78% |
6540* |
84% |
|
|
| Dapsone |
NA |
NA |
NA |
|
|
|
Sulphonamides | |||||
| Sulfadiazine |
NA |
NA |
NA |
|
|
| Sulfamethoxazole |
NA |
NA |
NA |
|
|
| Sulfadoxine |
NA |
NA |
NA |
|
|
|
Amino alcohols | |||||
| Halofantrine |
136 (66) |
135 (98) |
31.9 (11) |
1.0 |
0.2 |
| Lumefantrines |
137 (70) |
107 (137) |
2.07 (0.55) |
0.8 |
0.0 |
| Mefloquine (Racemic) |
158 (33) |
223 (120) |
100 (3.6) |
1.4 |
0.6 |
| Mefloquine (+ RS) |
133 (41) |
226 (76) |
134 (110) |
1.7 |
1.0 |
| Quinine sulfate |
217 (0.7) |
2110 (280) |
318 (180) |
9.7 |
1.5 |
|
Antibiotics | |||||
| Trimethoprim |
3740 (120) |
NA |
NA |
|
|
| Thiostrepton |
913 (210) |
959 (570) |
556 (58) |
1.1 |
0.6 |
| Clindamycin |
325 (64) |
NA |
NA |
|
|
| Cis-mirincamycin (HCl) |
NA |
NA |
64% |
|
|
| Trans-mirincamycin (HCl) |
86% |
NA |
66% |
|
|
| Tetracycline |
2270 (170) |
NA |
NA |
|
|
|
Other | |||||
| Fosmidomycin mono sodiums |
91% |
NA |
NA |
|
|
| Methylene blue trihydrate |
21.9 (0.07) |
280 (130) |
287 (100) |
12.8 |
13.1 |
| Pentamidine | 697 (36) | 1560 (620) | 2850 (540) | 2.2 | 4.1 |
ABS Asexual blood stage, gam gametocyte, a n = 2, b n = 3. IC50 nM (SD), * n = 1 only, NA Not active at 40 μM, % at 40 μM. sPotential solubility issues with stock compounds in DMSO.