Table 1.
Test Compounds | In Vitro W2 Strain | In Vivo P. berghei (ED50, mg/kg) | MCD (mg/kg) | MTD (mg/kg) | TIb |
---|---|---|---|---|---|
7 | 0.56 | 1.6 | 8.4 | 144 | 17 |
8 | 0.12 | 0.44 | 3.1 | 345 | 111 |
9 | 0.14 | 0.49 | 2.9 | 310 | 107 |
10 | 0.31 | 1.2 | 6.6 | 338 | 51 |
11 | 0.34 | 1.3 | 5.9 | 439 | 74 |
12 | 0.29 | 1.0 | 7.1 | 399 | 56 |
13 | 0.26 | 1.1 | 6.8 | 425 | 63 |
14 | 0.40 | 1.7 | 8.9 | 379 | 43 |
15 | 0.23 | 0.74 | 4.7 | 335 | 71 |
16 | 0.28 | 1.5 | 7.9 | 440 | 56 |
17 | 2.9 | 8.7 | 39 | 429 | 11 |
18 | 3.4 | 10 | 42 | 504 | 12 |
19 | 0.14 | 0.14 | 0.77 | 102 | 132 |
20 | 0.19 | 0.12 | 0.69 | 88 | 128 |
21 | 0.62 | 1.7 | 5.6 | 55 | 10 |
22 | 0.57 | 1.5 | 4.9 | 51 | 10 |
Febrifugine | 0.76 | 2.3 | 12 | 35 | 3 |
Chloroquine | 224 | 4.5 | 40.0 | 240 | 6 |
Antimalarial activities were determined after i.p. administration of the compounds once daily for 4 days to infected mice.
Therapeutic indices were calculated as MTD divided by MCD.