Krieg R Jortzik E Goetz AA Blandin S Wittlin S Elhabiri M Rahbari M Nuryyeva S Voigt K Dahse HM Brakhage A Beckmann S Quack T Grevelding CG Pinkerton AB Schönecker B Burrows J Davioud-Charvet E Rahlfs S Becker K 2017 In search of antiparasitic agents, we here identify arylmethylamino steroids as potent compounds and characterize more than 60 derivatives. The lead compound 1o is fast acting and highly active against intraerythrocytic stages of chloroquine-sensitive and resistant Plasmodium falciparum parasites (IC50 1-5 nM) as well as against gametocytes. In P. berghei-infected mice, oral administration of 1o drastically reduces parasitaemia and cures the animals. Furthermore, 1o 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, 1o has a remarkable activity against the blood-feeding trematode parasite Schistosoma mansoni. The steroid and the hydroxyarylmethylamino moieties are essential for antimalarial activity supporting a chelate-based quinone methide mechanism involving metal or haem bioactivation. This study identifies chemical scaffolds that are rapidly internalized into blood-feeding parasites. application/pdf https://sonar.ch/global/documents/176603 eng info:eu-repo/semantics/altIdentifier/doi/10.1038/ncomms14478 info:eu-repo/semantics/altIdentifier/pmid/28211535 info:eu-repo/semantics/openAccess Nature communications. - 2017 Amines Animals Anopheles Anti-Infective Agents Antiparasitic Agents Cell Death Cell Proliferation Female Germ Cells Inhibitory Concentration 50 Life Cycle Stages Malaria Mice Models, Biological Parasites Plasmodium berghei Plasmodium falciparum Schistosoma mansoni Steroids Toxicity Tests, Acute Arylmethylamino steroids as antiparasitic agents. http://purl.org/coar/resource_type/c_6501