NOVEL BISQUINOLINE ANTIMALARIALS - SYNTHESIS, ANTIMALARIAL ACTIVITY, AND INHIBITION OF HEME POLYMERIZATION

We report the synthesis of two series of novel bisquinoline compounds that inhibit the growth of both chloroquine-sensitive and chloroquine- resistant strains of Plasmodium falciparum. To study the molecular bas is of the action of these novel antimalarial drugs, we examined their ability to inhibit haem polymerisation in the presence and absence of parasite extracts. The level of antimalarial potency was correlated wi th the level of inhibition of haem polymerisation, suggesting that the se bisquinolines exert their antimalarial activity by antagonising the sequestration of toxic haem moieties.