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The lead compound <jats:bold>1o<\/jats:bold> is fast acting and highly active against intraerythrocytic stages of chloroquine-sensitive and resistant <jats:italic>Plasmodium falciparum<\/jats:italic> parasites (IC<jats:sub>50<\/jats:sub> 1\u20135\u2009nM) as well as against gametocytes. In <jats:italic>P. berghei-<\/jats:italic>infected mice, oral administration of <jats:bold>1o<\/jats:bold> drastically reduces parasitaemia and cures the animals. Furthermore, <jats:bold>1o<\/jats:bold> efficiently blocks parasite transmission from mice to mosquitoes. The steroid compounds show low cytotoxicity in mammalian cells and do not induce acute toxicity symptoms in mice. Moreover, <jats:bold>1o<\/jats:bold> has a remarkable activity against the blood-feeding trematode parasite <jats:italic>Schistosoma mansoni<\/jats:italic>. 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