TABLE 1.
Compounda | Mol wt | ID50
|
TD50
|
TI | ||
---|---|---|---|---|---|---|
μg/ml | μM | μg/ml | μM | |||
Artemisinin | 282.34 | 2.3 | 8.0 | >320b | >1,130 | ≥243 |
Artemether | 298.4 | 0.2 | 0.7 | 220 | 740 | 1,100 |
2d | 464.68 | 0.5 | 1.1 | 160 | 340 | 320 |
2c | 509.43 | 0.6 | 1.2 | >320b | >630 | ≥933 |
2b | 430.54 | 0.6 | 1.4 | >320b | >740 | ≥933 |
2a | 326.43 | 2.7 | 8.3 | 510 | 1,560 | 190 |
Deoxy-2a | 310.43 | 173 | 560 | 200 | 640 | 1.2 |
Trimethoprim | 290.3 | 5.2 | 17.9 | 60 | 210 | 12 |
The parent compound is shown first followed by the known derivative. The five new derivatives are listed in decreasing order of efficacy according to concentrations in μg/ml.
Toxicity endpoint was not reached; a value 1/4 log greater than the concentration tested was used to compute the TI.