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Arylmethylamino steroids as antiparasitic agents

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10.1038_ncomms14478.pdf (1.172Mb)
Date
2017
Author
Krieg, Reimar
Jortzik, Esther
Goetz, Alice-Anne
Blandin, Stéphanie
Wittlin, Sergio
Elhabiri, Mourad
Rahbari, Mahsa
Nuryyeva, Selbi
Voigt, Kerstin
Dahse, Hans-Martin
Brakhage, Axel
Beckmann, Svenja
Quack, Thomas
Grevelding, Christoph G.
Pinkerton, Anthony B.
Schönecker, Bruno
Burrows, Jeremy
Davioud-Charvet, Elisabeth
Rahlfs, Stefan
Becker, Katja
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http://dx.doi.org/10.22029/jlupub-8658
Abstract

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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https://doi.org/10.1038/ncomms14478
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