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Arylmethylamino steroids as antiparasitic agents. 2017
Reimar Krieg, and
Esther Jortzik, and
Alice-Anne Goetz, and
Stéphanie Blandin, and
Sergio Wittlin, and
Mourad Elhabiri, and
Mahsa Rahbari, and
Selbi Nuryyeva, and
Kerstin Voigt, and
Hans-Martin Dahse, and
Axel Brakhage, and
Svenja Beckmann, and
Thomas Quack, and
Christoph G Grevelding, and
Anthony B Pinkerton, and
Bruno Schönecker, and
Jeremy Burrows, and
Elisabeth Davioud-Charvet, and
Stefan Rahlfs, and
Katja Becker
Institute of Anatomy II, University Hospital Jena, Teichgraben 7, 07743 Jena, Germany.
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.
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