Plasmepsin II inhibition and antiplasmodial activity of Primaquine–Statine `double-drugs'

Statine-based inhibitors of Plasmepsin II (PLMII) coupled with Primaquine have been designed using the `double-drug'' approach. The IC50 values for PLMII inhibition ranged from 0.59 to 400 nM and the best IC50 value for inhibition of Plasmodium falciparum growth in vitro was 0.4 μM, which represent a remarkable improvement compared to other statine-based PLMII inhibitors. [Copyright &y& Elsevier]