A series of novel low molecular weight compounds with high activity against Plasmodium falciparum have been developed, synthesized and tested. The compounds are based on a substituted steroidal pharmacophor and are as antiinfective agents in their structure completely new. The compounds are highly active against red blood cell stages of P. falciparum, also of chloroquine-resistant parasites. Present SAR data indicate that the hydrophobic steroid component and a hydroxyarylmethylamino group are essential for the antimalarial action of the compounds. The hydrophobic steroid part is likely to mediate membrane permeability.
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