Table 5.
Example of benzimidazole phthalimide hybrids 5a-e and their antimalarial activity.
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---|---|---|---|---|---|---|
Compound | 3D7 IC50a | RKL-9 IC50a | SIb | |||
- | R | R1 | R2 | - | - | - |
5a | CH3 | CH2CH(CH3)2 | 4-Cl-phenyl | 0.74 | 1.71 | >135 >675 |
5b | H | CH(CH3)CH2CH3 | 4-CF3-phenyl | 0.64 | 1.62 | >156 >781 |
5c | H | CH(CH3)CH2CH3 | benzyl | 0.81 | 1.88 | >123 >617 |
5d | CH3 | CH(CH3)CH2CH3 | 4-F-phenyl | 2.2 | 3.43 | >46 >227 |
5e | H | CH(CH3)2 | 4-CF3-phenyl | 2.3 | 3.92 | >43 |
Note: aIC50 (µM): compound concentration that reduced the parasite load by 50%. bSI: selectivity index (CC50/IC50). P. falciparum 3D7 sensitive and RKL-9 CQ resistant strains.