Table 5.
In vitro activity of WR7930-related compounds against NTS and adult S. mansoni and its in vivo effect on S. mansoni in infected NMRI mice treated with an oral dosage of 100 mg/kga
| Treatment group |
In vitro IC50 (SD) [μM] |
In vivo |
|||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|
| NTS | Adult worms | No. of mice investigated | No. of mice cured | Mean no. of worms (SD) |
TWR (%) | P value | FWBR (%) | P value | |||
| Liver | Mesenteric veins | Total | |||||||||
| Control | 9 | 2.0 (3.5) | 27.0 (27.7) | 29.0 (28.5) | |||||||
| Compound 12 | 5.7 (3.3) | 27.9 (6.8) | 4 | 0 | 1.5 (1.0) | 5.8 (2.6) | 7.3 (2.8) | 75.0 | 0.31 | 83.1 | 0.18 |
| Compound 13 | 4.3 (2.2) | 3.9 (0.7) | 4 | 0 | 2.8 (2.8) | 3.3 (2.5) | 5.3 (1.5) | 81.9 | 0.12 | 93.0 | 0.02 |
a
In vitro experiments were carried out 3 times in duplicate for NTS (n = 6) and 3 times for adult schistosomes (n = 3) for each tested drug. SD, standard deviation; TWR, total worm burden reduction; FWBR, female worm burden reduction.