Table 1. Antischistosomal activities of some hits identified through phenotypic screening of the MMV malaria, stasis and pathogen boxes.
| Compound |
S. mansoni IC50
a
(μM) |
Adult S. mansoni b (% WBR) | Compound |
S. mansoni IC50
a
(μM) |
Adult S. mansoni b (% WBR) | Adult S. haematobium effect (%), 10 μM, 72 h | ||
| NTS | Adult | NTS | Adult | |||||
| 40 | 4.7 | 0.8 | 52.5 | 54 | 7.2 | 7.5 | 51.6 | — |
| 41 | 2.7 | 0.8 | 0 | 55 | 1.7 | 7.0 | — | — |
| 42 | 1.8 | 3.4 | 1.8 | 56 | 0.8 | 3.0 | — | 100.0 |
| 43 | 3.4 | 6.3 | 18.7 | 57 | 0.6 | 2.0 | 70.7 | 100.0 |
| 44 | — | 0.8 | 40.8 | 58 | 2.6 | 3.0 | 67.8 | 75.4 |
| 45 | 3.5 | 2.5 | 0 | 59 | 0.9 | 6.8 | — | 87.7 |
| 46 | 0.6 | 2.0 | 0 | 60 | 0.8 | 4.7 | — | 75.4 |
| 47 | 1.2 | 2.7 | 12.2 | 61 | 0.2 | 2.1 | — | 100.0 |
| 48 | 1.5 | 2.6 | 3.2 | 62 | 0.4 | 3.7 | 55.2 | 90.8 |
| 49 | 2.1 | 2.0 | 35.9 | 63 | 0.4 | 2.5 | — | 100.0 |
| 50 | 6.3 | 3.1 | 0 | 64 | 2.2 | 3.4 | — | 75.4 |
| 51 | 0.7 | 3.7 | 10.0 | 65 | 2.9 | 4.9 | 22.4 | 82.5 |
| 52 | 0.9 | 2.2 | — | 66 | 16.7 | 7.9 | 32.8 | 50.9 |
| 53 | 0.5 | 2.9 | 0 | |||||
aIC50 after 72 h.
b In vivo studies in mice: 400 mg kg–1 single oral dose for 40–44 and 200 mg kg–1 single oral dose for 45–66.