TABLE 1.
Iron-chelating and in vitro antimalarial activities of synthesized conjugated hydrazone derivatives
| Compound | Activity (mean concn [μM] ± SEM)a |
|
|---|---|---|
| Iron-chelating activity | In vitro antimalarial activity | |
| 1a | 83.86 ± 5.30 | NA |
| 1b | 75.24 ± 8.57 | NA |
| 1c | >100 | NA |
| 1d | >100 | 59.48 ± 9.55 |
| 1e | 11.73 ± 2.73 | 71.33 ± 6.93 |
| 1f | 9.73 ± 1.89 | 42.96 ± 3.63 |
| 2a | 83.66 ± 9.33 | NA |
| 2b | >100 | NA |
| 2c | >100 | NA |
| 2d | >100 | 62.16 ± 8.54 |
| 2e | 13.90 ± 2.82 | 78.85 ± 7.22 |
| 2f | 15.12 ± 4.15 | 65.56 ± 4.91 |
| 3a | 65.24 ± 10.95 | NA |
| 3b | 53.58 ± 7.30 | NA |
| 3c | >100 | NA |
| 3d | >100 | >100 |
| 3e | 8.94 ± 3.14 | >100 |
| 3f | 12.26 ± 4.63 | 89.44 ± 10.74 |
| 4a | 21.37 ± 4.15 | NA |
| 4b | 12.48 ± 1.68 | NA |
| 4c | >100 | NA |
| 4d | >100 | 92.98 ± 6.93 |
| 4e | 2.45 ± 0.99 | >100 |
| 4f | 2.51 ± 1.97 | 76.55 ± 9.16 |
| 5a | 8.28 ± 3.22 | >100 |
| 5b | 6.10 ± 1.81 | NA |
| 5c | 43.73 ± 5.89 | NA |
| 5d | 78.11 ± 8.25 | 27.11 ± 2.87 |
| 5e | 2.35 ± 0.35 | 53.87 ± 4.32 |
| 5f | 1.87 ± 0.24 | 16.95 ± 1.19 |
| Deferoxamine | 0.72 ± 0.19 | 27.13 ± 2.03 |
| Chloroquine | ND | 0.020 ± 0.0012 |
| Artesunate | ND | 0.015 ± 0.0009 |
a
Values indicate the means (± the standard errors of the means, where applicable) of a single parallel determination performed in triplicate. Iron-chelating activity was determined as a 50% decrease in TPTZ-Fe(II) absorbance. In vitro antimalarial activity was determined using a SYBR green assay and is expressed as the IC50. NA, not applicable; ND, not determined.