Antiplasmodial activity of chloroquine analogs against chloroquine-resistant parasites, docking studies and mechanisms of drug action

Table 1 Activity of CQ and CQAn against P . falciparum (IC ₅₀ ) CQ-R (W2) or CQ-S (3D7) parasites

Molecule	Chemical structure	Anti- P. falciparum activity (IC₅₀in μM)*
Molecule	Chemical structure	W2( CQ- R)	3D7l( CQ- S)
CQAn28		0.71 ± 0.03	14.87 ± 3.58
CQAn33		0.02 ± 0.001	1.17 ± 0.10
CQAn34		0.23 ± 0.15	0.3 ± 0.01
CQAn37		0.07 ± 0.03	0.57 ± 0.24
CQAn39		0.64 ± 0.29	2.39 ± 0.11
CQAn45		0.77 ± 0.21	1.17 ± 0.00
Chloroquine		0.38±0.03	0.081 ± 0.019

*Average ± SD of the IC₅₀ is based in two to four experiments performed with each parasite strain using anti-HRPII method.

ISSN: 1475-2875