Table 2. Half-Maximal Inhibitory Concentration (IC50) and Inhibition Constant (Ki) Values of N-Acyl Inhibitors Assayed Against P. falciparum IspC.
| compound | R1 | R2 | IC50 (μM) | Kia (μM) | Kib (μM) |
|---|---|---|---|---|---|
| 1a = fosmidomycin | Na/H | H | 0.03412 | ND | NA |
| 2a = FR900098 | Na/H | CH3 | 0.02412 | 0.009 | NA |
| 3a | Na/H | n-butyl | 2.448 | 0.860 | NA |
| 4a | Na/H | CH2(CH2)2Ph | 1.344 | 0.470 | NA |
| 1b | Na/H | CH2CH2Ph | 1.309 | 0.338 | NA |
| 2b | Na/H | CH2(CH2)2Ph | 0.900 | 0.162 | NA |
a
Relative to DXP.
b
Relative to NADPH; ND = not determined; NA = not applicable. The inhibition constant (Ki) values are the results of the mechanism of inhibition (MoI) enzymatic assays performed at least in triplicate.