Table 2.
Inhibition of purified Dxr from Plasmodium falciparum by members of the phosphonate library.
| Substrate | IC50 (nM) (mean ± SD) | KI (nM) (mean ± SD) |
|---|---|---|
| FR-900098 | 15 ± 3 | 3.2 ± 1.0 |
| FR-33289 | 16 ± 3 | 3.0 ± 0.8 |
| Fosmidomycin | 36 ± 6 | 6.8 ± 1.6 |
| Hydroxyfosmidomycin | 41 ± 5 | 7.1 ± 1.4 |
| FR-900098-OMe | NI | NI |
| FR-33289-OMe | NI | NI |
| Fosmidomycin-OMe | NI | NI |
| Hydroxyfosmidomycin-OMe | NI | NI |
NI: no enzyme inhibition detected; SD: standard deviation