Table 3.
Structures and antimalarial activity of benzimidazole derivatives 3a-e.
| |||||
|---|---|---|---|---|---|
| Compound | 3D7 IC50a | Dd2 IC50a | bCam3.IIrev IC50a | cCam3.IIC580Y IC50a | Dd2-SJ Resistant IC50a |
| 3a, R = H | 77 | 97.3 | 350 | 264 | 46 |
| 3b, R = CH3 | 42 | 31.7 | 140 | 81 | 17.5 |
| 3c, R = OCH3 | 43 | - | 212 | 168 | - |
| 3d, R = 3,5-di-CH3 | 23 | - | 133 | 139 | - |
| 3e, R = 4,5-di-OCH3 | 6.4 | - | 47 | 63 | - |
Note: aIC50 (nM): compound concentration that reduced the parasite load of 50%. bCam3.II line has a K13 R539T mutation that is in Cam3.IIrev was gene-edited to wild type K13 gene. cCam3.II lines bearing the C580Y mutation in the K13 gene, which is responsible for resistance to artemisinin.