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. 2024 Feb 26;31(15):1955–1982. doi: 10.2174/0929867331666230915093928

Table 3.

Structures and antimalarial activity of benzimidazole derivatives 3a-e.

graphic file with name CMC-31-1955-T3.jpg
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.