Table 1.
MIC and Ki values of the substrates 6a–h and 11a–c against B. anthracis.
| Compound | MIC (μg/mL) | Ki (nM) ± SEM |
|---|---|---|
| B. anthracis | B anthracis DHFR | |
| TMP | >128 * | ~8,770 * |
| RAB1 | 2–4 * | 9.4 ± 0.2 * |
| 6a | 2.0 | 8.8 ± 0.2 |
| 6b | 1.0 | 6.8 ± 0.2 |
| 6c | 2–4 | 7.9 ± 0.2 |
| 6d | 4 | 10.4 ± 0.2 |
| 6e | 0.5 | 4.9 ± 0.2 |
| 6f | 4 | 5.9 ± 0.2 |
| 6g | 4 | 8.4 ± 0.2 |
| 6h | 4 | 9.0 ± 0.2 |
| 11a | 8 | 59.0 ± 0.9 |
| 11b | 8 | 24.9 ± 0.3 |
| 11c | 8 | 20.0 ± 0.3 |
* Indicates previously published data: TMP [8]; RAB1 [9,10,12,15,16]; Ki = 50% inhibition normalized for the intrinsic affinity for the substrate, as outlined in the Cheng-Prusoff formalism [20]. SEM = standard error of the mean. MIC values report the range of values from two independent experiments performed in duplicate. Ki values report the mean from at least three independent measurements.