Abstract

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 μg/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.

Keywords: Synthesis, Antimalarial activity, Plasmodium berghei, Quinoline, Chloroquine, Mercaptopurine, Anopheles mosquitoes, P. Falciparum, Plasmodium strains, de novo drug design, chemical modification, Thiopurines, immunosupressors, 6-mercaptopurine derivates, HRMS ESI