Table 1.
The anti-P. falciparum activities of BAQ and MAQ determined in parallel with chloroquine, by the ELISA anti-HRPII assay or by 3H hypoxanthine incorporation.
Table 2.
Cytotoxicity of BAQ and MAQ against a human hepatoma cell line (HEPG2) and a monkey kidney cell line (BGM) determined by the MTT assay.
Table 3.
Antimalarial activity of BAQ and MAQ in mice infected with P. berghei after treatment with daily doses of the compounds during three consecutive days.
Figure 1.
Inhibition of hemozoin formation by the CQ analogs BAQ and MAQ (mean ± SD from triplicates), in two different experiments.
Statistical differences as compared to drug-free controls are indicated in each graph by an asterisk (p<0.05). The p and r values represent the statistical correlation analyses.
Figure 2.
Chemical structures of the protonated forms of the CQ analogs BAQ and MAQ.
Figure 3.
Compounds docked in dimeric hematin.
(A) Protonated CQ, (B) MAQ-1, (C) MAQ-2, (D) MAQ-3, (E) BAQ-1, (F) BAQ-2.
Table 4.
Docking energies of the protonated forms of the CQ analogs BAQ and MAQ.
Figure 4.
Best conformations of the protonated forms of chloroquine, MAQ and BAQ (in green) in the binding pocket of NADH (in CPK) as generated by the MVD® software.
(A) Protonated chloroquine, (B) MAQ-1, (C) MAQ-2, (D) MAQ-3, (E) BAQ-1, (F) BAQ-2.
Table 5.
Docking results of NADH and the protonated forms of chloroquine, BAQ and MAQ in the active site of PfLDH.