Synthesis and In Vivo Antimalarial Activity of Quinoline/Mercaptopurine Conjugates

In this paper we describe the preparation, characterization and antimalarial activity in vivo of novel quinoline/mercatopurine conjugates. The compounds were tested in vivo in a murine model using chloroquine as a reference compound. The values of inhibition of parasite multiplication relative to chloroquine were determined and the compound 4-(6'-mercatopurine)-7-chloroquinoline was considered statistically identical to chloroquine at the same dosage. The compounds were not cytotoxic at the maximum concentration used (100 mu g/mL). Possible mechanisms of action are discussed. In light of these data, the title compounds may serve as prototypes for the development of novel antimalarial agents.