Table 2. In VitroP. falciparum Growth Inhibition of Acid and Amide Variants of 7e.
| Compound | X | R | EC50 (nM)a |
|---|---|---|---|
| 7e·HCl | NH | (CH2)2NHMe·HCl | 108 ± 7 |
| 14e | O | Me | >10,000 |
| 15e | O | H | >10,000 |
| 16e | NH | Me | >10,000 |
| 17e | NH | (CH2)2OH | 3,270 ± 40 |
| 18e | NH | (CH2)3CH3 | 1,020 ± 20 |
| 19e·HCl | NH | (CH2)2NH2·HCl | 263 ± 25 |
| 20e·HCl | NH | (CH2)2NMe2·HCl | 264 ± 26 |
| 21e·HCl | NH | (CH2)3NH2·HCl | 726 ± 57 |
| 22e·HCl | NH | (CH2)3NHMe·HCl | 217 ± 28 |
| 23e·HCl | NH | (CH2)3NMe2·HCl | 240 ± 23 |
a
Growth inhibition (72 h) of asexual blood stages determined using SYBR Green I assay. Values represent average ± SEM from at least three independent biological replicates. The Dd2 strain is resistant to chloroquine, pyrimethamine, and mefloquine.