Synthesis and In Vivo Antimalarial Activity of Novel Derivatives of 6- Mercaptopurine

Chloroquine has been widely used to treat malaria, however, it is currently largely ineffective due to widespread parasite resistance. In this work, five 6-mercaptopurine derivates were synthesized and their in vivo antimalarial activity was examined. Among the three derivates of 6-mercaptopurine containing 1,2,3-triazole, compound 16 stands out, which showed increased activity over the days analyzed, inhibiting the growth of parasites in a way similar or even superior to chloroquine. Also, among the derivates of 6-mercaptopurine containing steroid, the analog 18 exhibited suppression of parasitaemia close to that of chloroquine. None of compounds showed cytotoxicity against mammalian cells.