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dc.contributor.authorCabrera, Diego Gonzalez
dc.contributor.authorLe Manach, Claire
dc.contributor.authorDouelle, Frederic
dc.contributor.authorYounis, Yassir
dc.contributor.authorFeng, Tzu-Shean
dc.contributor.authorPaquet, Tanya
dc.contributor.authorNchinda, Aloysius T
dc.contributor.authorStreet, Leslie J
dc.contributor.authorTaylor, Dale
dc.contributor.authorde Kock, Carmen
dc.contributor.authorWiesner, Lubbe
dc.contributor.authorDuffy, Sandra
dc.contributor.authorWhite, Karen L
dc.contributor.authorZabiulla, K Mohammed
dc.contributor.authorSambandan, Yuvaraj
dc.contributor.authorBashyam, Sridevi
dc.contributor.authorWaterson, David
dc.contributor.authorWitty, Michael J
dc.contributor.authorCharman, Susan A
dc.contributor.authorAvery, Vicky M
dc.contributor.authorWittlin, Sergio
dc.contributor.authorChibale, Kelly
dc.date.accessioned2018-03-07T12:30:24Z
dc.date.available2018-03-07T12:30:24Z
dc.date.issued2014
dc.identifier.issn0022-2623
dc.identifier.doi10.1021/jm401760c
dc.identifier.urihttp://hdl.handle.net/10072/102413
dc.description.abstractA novel series of 2,4-diaminothienopyrimidines with potential as antimalarials was identified from whole-cell high-throughput screening of a SoftFocus ion channel library. Synthesis and structure–activity relationship studies identified compounds with potent antiplasmodial activity and low in vitro cytotoxicity. Several of these analogues exhibited in vivo activity in the Plasmodium berghei mouse model when administered orally. However, inhibition of the hERG potassium channel was identified as a liability for this series.
dc.description.peerreviewedYes
dc.languageEnglish
dc.language.isoeng
dc.publisherAmerican Chemical Society
dc.publisher.placeUnited States
dc.relation.ispartofpagefrom1014
dc.relation.ispartofpageto1022
dc.relation.ispartofissue3
dc.relation.ispartofjournalJournal of Medicinal Chemistry
dc.relation.ispartofvolume57
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.title2,4-Diaminothienopyrimidines as orally active antimalarial agents
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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