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
Keywords: Antimalarial activities, Chemotherapy, Click chemistry, STEROIDS, 6-thiopurine, 1, 2, 3-triazole.
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