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Arylmethylamino steroids as antiparasitic agents

dc.contributor.authorKrieg, Reimar
dc.contributor.authorJortzik, Esther
dc.contributor.authorGoetz, Alice-Anne
dc.contributor.authorBlandin, Stéphanie
dc.contributor.authorWittlin, Sergio
dc.contributor.authorElhabiri, Mourad
dc.contributor.authorRahbari, Mahsa
dc.contributor.authorNuryyeva, Selbi
dc.contributor.authorVoigt, Kerstin
dc.contributor.authorDahse, Hans-Martin
dc.contributor.authorBrakhage, Axel
dc.contributor.authorBeckmann, Svenja
dc.contributor.authorQuack, Thomas
dc.contributor.authorGrevelding, Christoph G.
dc.contributor.authorPinkerton, Anthony B.
dc.contributor.authorSchönecker, Bruno
dc.contributor.authorBurrows, Jeremy
dc.contributor.authorDavioud-Charvet, Elisabeth
dc.contributor.authorRahlfs, Stefan
dc.contributor.authorBecker, Katja
dc.date.accessioned2022-11-18T09:51:43Z
dc.date.available2017-05-24T14:06:09Z
dc.date.available2022-11-18T09:51:43Z
dc.date.issued2017
dc.description.abstractIn 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.en
dc.identifier.urihttp://nbn-resolving.de/urn:nbn:de:hebis:26-opus-128473
dc.identifier.urihttps://jlupub.ub.uni-giessen.de//handle/jlupub/9270
dc.identifier.urihttp://dx.doi.org/10.22029/jlupub-8658
dc.language.isoende_DE
dc.rightsNamensnennung 4.0 International*
dc.rights.urihttps://creativecommons.org/licenses/by/4.0/*
dc.subject.ddcddc:630de_DE
dc.titleArylmethylamino steroids as antiparasitic agentsen
dc.typearticlede_DE
local.affiliationZentrende_DE
local.opus.fachgebietIFZ Interdisziplinäres Forschungszentrum für Umweltsicherungde_DE
local.opus.id12847
local.opus.instituteBiochemistry and Molecular Biologyde_DE
local.source.freetextNature Communications 8:14478de_DE
local.source.urihttps://doi.org/10.1038/ncomms14478

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