Table 4. Antischistosomal properties of some promising compounds.
Compound a | Species | Life cycle stage | In vitro b (μM) | In vivo c (% WBR) | Morphological effect (≤100 μM in ≤72 h) |
Enzyme inhibition (IC50, μM) | |||
Worm death (%) | Tegument damage d (%) | Motor activity d (%) | Egg d (% reduction) | ||||||
155 162 | S. mansoni | Adult | 53.5 | 100 | 25 | 100 | |||
156 163,164 | S. mansoni | Juvenile | 50.2 | ||||||
Adult | 70.0 | 100 | 100 | 100 | 80.0 | ||||
157 165,166 | S. mansoni | Juvenile | 58.0 | ||||||
Adult | 60.6 | 100 | 100 | 100 | 64.1 | ||||
158 167 | S. mansoni | Adult | 100 | 100 | 100 | ||||
159 168 | S. mansoni | Larva | 88.6 | ||||||
Juvenile | 68.3 | ||||||||
Adult | 70.6 | ||||||||
S. japonicum | Larva | 90.0 | |||||||
Juvenile | 59.9 | ||||||||
Adult | 53.2 | ||||||||
160 169 | S. mansoni | Adult | 100 | Y | EC50 = 8.8 μM | EC50 = 3.6 μM | SmAChE e | ||
161 170 | B. glabrata | Snail | 1.2 | ||||||
162 171 | S. mansoni | Miracidia | 99.7 | ||||||
Cercariae | 41.0 | ||||||||
163 172,173 | S. mansoni | Adult | 81.2 | 100 | 20 | 100 | 54–67 | SmTGR | |
164 174 | S. japonicum | Larva | 12.8 | ||||||
Adult | 15.6 | Y | |||||||
165 175 | S. mansoni | Adult | 83.3 | Y | Y | Y | |||
166 176 | S. mansoni | Larva | 2.6 | SmTGR | |||||
Adult | 4.9 | ||||||||
167 177 | S. mansoni | Larva | 13.9 | ||||||
Adult | 100 | Y | |||||||
168 178 | S. mansoni | rSmNACE f (2.2) | |||||||
nSmNACE g (20) | |||||||||
169 179 | S. mansoni | Adult | 47.9 | Y | |||||
170 180 | S. mansoni | Adult | 100 | SmTGR |
aReference.
bIC50/LC50.
cTotal worm burden reduction.
dSignificant effect observed.
e S. mansoni acetylcholinesterase.
fRecombinant S. mansoni NAD catabolizing enzyme.
gNative S. mansoni NAD catabolizing enzyme.