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3-Hydroxy-N'-arylidenepropanehydrazonamides with Halo-Substituted Phenanthrene Scaffolds Cure P. berghei Infected Mice When Administered Perorally

dc.contributor.authorLeven, Michael
dc.contributor.authorKnaab, Tanja C
dc.contributor.authorHeld, Jana
dc.contributor.authorDuffy, Sandra
dc.contributor.authorMeister, Stephan
dc.contributor.authorFischli, Christoph
dc.contributor.authorMeitzner, Diane
dc.contributor.authorLehmann, Ursula
dc.contributor.authorLungerich, Beate
dc.contributor.authorKuna, Krystina
dc.contributor.authorStahlke, Petra
dc.contributor.authorDelves, Michael
dc.contributor.authorBuchholz, Mirko
dc.contributor.authorWinzeler, Elizabeth A
dc.contributor.authorAvery, Vicky M
dc.contributor.authorMordmueller, Benjamin
dc.contributor.authorWittlin, Sergio
dc.contributor.authorKurz, Thomas
dc.date.accessioned2018-01-23T01:00:52Z
dc.date.available2018-01-23T01:00:52Z
dc.date.issued2017
dc.identifier.issn0022-2623
dc.identifier.doi10.1021/acs.jmedchem.7b00140
dc.identifier.urihttp://hdl.handle.net/10072/351638
dc.description.abstractStructural optimization of 3-hydroxy-N′-arylidenepropanehydrazonamides provided new analogs with nanomolar to subnanomolar antiplasmodial activity against asexual blood stages of Plasmodium falciparum, excellent parasite selectivity, and nanomolar activity against the earliest forms of gametocyte development. Particularly, derivatives with a 1,3-dihalo-6-trifluoromethylphenanthrene moiety showed outstanding in vivo properties and demonstrated in part curative activity in the Plasmodium berghei mouse model when administered perorally.
dc.description.peerreviewedYes
dc.languageEnglish
dc.publisherAmerican Chemical Society
dc.relation.ispartofpagefrom6036
dc.relation.ispartofpageto6044
dc.relation.ispartofissue14
dc.relation.ispartofjournalJournal of Medicinal Chemistry
dc.relation.ispartofvolume60
dc.subject.fieldofresearchMedicinal and Biomolecular Chemistry not elsewhere classified
dc.subject.fieldofresearchMedicinal and Biomolecular Chemistry
dc.subject.fieldofresearchOrganic Chemistry
dc.subject.fieldofresearchPharmacology and Pharmaceutical Sciences
dc.subject.fieldofresearchcode030499
dc.subject.fieldofresearchcode0304
dc.subject.fieldofresearchcode0305
dc.subject.fieldofresearchcode1115
dc.title3-Hydroxy-N'-arylidenepropanehydrazonamides with Halo-Substituted Phenanthrene Scaffolds Cure P. berghei Infected Mice When Administered Perorally
dc.typeJournal article
dc.type.descriptionC1 - Articles
dc.type.codeC - Journal Articles
gro.hasfulltextNo Full Text
gro.griffith.authorDuffy, Sandra
gro.griffith.authorAvery, Vicky M.


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