TABLE 1

Inhibition by diastereomers of MMV-08138 of parasite growth and PfIspD enzyme activity

StereoisomerParasite growth (EC50 [μM]) under indicated conditionsPfIspD activity (IC50 [μM])a
No rescuea+IPP
1S,3S>50b>50b>25c
1R,3S0.11 (0.10–0.12)>25c0.0071 (0.0061–0.0083)
1R,3R3.8 (2.7–5.3)>25c0.17 (0.14–0.20)
1S,3R18.6 (12.4–28.0)>25c2.5 (1.9–3.1)
  • a Values represent means (95% confidence intervals).

  • b No inhibition was observed at 50 μM, the highest concentration tested.

  • c Estimated value based on observation of partial inhibition.