TABLE 1

Calculated in vitro IC50sand IC90s of racemic and enantiomeric PZQ and 4-OH metabolites against adult S. mansoni at 4 and 72 h postincubation

CompoundIC50 (μg/ml) atIC90 (μg/ml) at 72 hEudysmic ratio
4 h72 h
Rac-PZQ0.10.050.4
R-PZQ0.040.020.04293
S-PZQ5.75.917.9
Rac-trans-4-OH-PZQ16.77.93,694a
R-trans-4-OH-PZQ13.44.158.4
S-trans-4-OH-PZQNAbNANA
Rac-cis-4-OH-PZQ15.84.881.4
R-cis-4-OH-PZQ4.52.448.7
S-cis-4-OH-PZQNANANA
  • a Extrapolated value determined by CompuSyn.

  • b NA, not active at 100 μg/ml.