TABLE 2

In vitro IC50s and IC90s of racemic and enantiomeric PZQ and 4-OH metabolites against NTS at 72 h postincubation

CompoundIC50 (μg/ml) at 72 hIC90 (μg/ml) at 72 hEudysmic ratio
Rac-PZQ1.534.5
R-PZQ0.0318.81,196
S-PZQ40.0522a
Rac-trans-4-OH-PZQ133a5,852a
R-trans-4-OH-PZQ28.5747
S-trans-4-OH-PZQNAbNA
Rac-cis-4-OH-PZQ911a2,448,837a
R-cis-4-OH-PZQ34.31,161a
S-cis-4-OH-PZQNANA
  • a Extrapolated value determined by CompuSyn.

  • b NA, not active at 100 μg/ml.