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dc.contributor.authorBarnes, Emmaen_US
dc.contributor.authorChoomuenwai, Vanidaen_US
dc.contributor.authorAndrews, Katherineen_US
dc.contributor.authorQuinn, Ronalden_US
dc.contributor.authorDavis, Rohanen_US
dc.date.accessioned2017-04-24T08:40:23Z
dc.date.available2017-04-24T08:40:23Z
dc.date.issued2012en_US
dc.date.modified2013-06-07T04:37:27Z
dc.identifier.issn14770539en_US
dc.identifier.doi10.1039/c2ob00029fen_US
dc.identifier.urihttp://hdl.handle.net/10072/48207
dc.description.abstractThe plant-derived natural product 14-hydroxy-6,12-muuroloadien-15-oic acid (1) was identified as a unique scaffold that could be chemically elaborated to generate novel lead- or drug-like screening libraries. Prior to synthesis a virtual library was generated and prioritised based on drug-like physicochemical parameters such as log P, log D5.5, hydrogen bond donors/acceptors, and molecular weight. The natural product scaffold (1) was isolated from the endemic Australian plant Eremophila mitchellii and then utilised in the parallel solution-phase generation of two series of analogues. The first library consisted of six semi-synthetic amide derivatives, whilst the second contained six carbamate analogues. These libraries have been evaluated for antimalarial activity using a chloroquine-sensitive Plasmodium falciparum line (3D7) and several compounds displayed low to moderate activity with IC50 values ranging from 14 to 33 卮en_US
dc.description.peerreviewedYesen_US
dc.description.publicationstatusYesen_US
dc.languageEnglishen_US
dc.language.isoen_US
dc.publisherRSC Publishingen_US
dc.publisher.placeUnited Kingdomen_US
dc.relation.ispartofstudentpublicationNen_US
dc.relation.ispartofpagefrom4015en_US
dc.relation.ispartofpageto4023en_US
dc.relation.ispartofissue20en_US
dc.relation.ispartofjournalOrganic & Biomolecular Chemistryen_US
dc.relation.ispartofvolume10en_US
dc.rights.retentionYen_US
dc.subject.fieldofresearchBiologically Active Moleculesen_US
dc.subject.fieldofresearchcode030401en_US
dc.titleDesign and synthesis of screening libraries based on the muurolane natural product scaffolden_US
dc.typeJournal articleen_US
dc.type.descriptionC1 - Peer Reviewed (HERDC)en_US
dc.type.codeC - Journal Articlesen_US
gro.facultyGriffith Sciences, School of Natural Sciencesen_US
gro.date.issued2012
gro.hasfulltextNo Full Text


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