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dc.contributor.authorRudrawar, Santosh
dc.contributor.authorDyason, Jeffrey C
dc.contributor.authorMaggioni, Andrea
dc.contributor.authorThomson, Robin J
dc.contributor.authorvon Itzstein, Mark
dc.date.accessioned2017-05-03T16:05:46Z
dc.date.available2017-05-03T16:05:46Z
dc.date.issued2013
dc.date.modified2014-03-27T03:59:49Z
dc.identifier.issn0968-0896
dc.identifier.doi10.1016/j.bmc.2013.05.054
dc.identifier.urihttp://hdl.handle.net/10072/57319
dc.description.abstractNovel 3,4-disubstituted-Neu5Ac2en derivatives have been synthesised to probe the open 150-loop conformation of influenza virus sialidases. Both equatorially and axially (epi) substituted C4 amino and guanidino 3-(p-tolyl)allyl-Neu5Ac2en derivatives were prepared, via the 4-epi-hydroxy derivative. The equatorially-substituted 4-amino derivative showed low micromolar inhibition of both group-1 (pdm09 H1N1) and group-2 (pdm57 H2N2) sialidases, and provides the first in vitro evidence that a group-2 sialidase may exhibit 150-loop flexibility.
dc.description.peerreviewedYes
dc.description.publicationstatusYes
dc.languageEnglish
dc.language.isoeng
dc.publisherPergamon
dc.publisher.placeUnited Kingdom
dc.relation.ispartofstudentpublicationN
dc.relation.ispartofpagefrom4820
dc.relation.ispartofpageto4830
dc.relation.ispartofissue16
dc.relation.ispartofjournalBioorganic Medicinal Chemistry
dc.relation.ispartofvolume21
dc.rights.retentionY
dc.subject.fieldofresearchMedicinal and biomolecular chemistry
dc.subject.fieldofresearchBiologically active molecules
dc.subject.fieldofresearchOrganic chemistry
dc.subject.fieldofresearchPharmacology and pharmaceutical sciences
dc.subject.fieldofresearchBiochemistry and cell biology
dc.subject.fieldofresearchcode3404
dc.subject.fieldofresearchcode340401
dc.subject.fieldofresearchcode3405
dc.subject.fieldofresearchcode3214
dc.subject.fieldofresearchcode3101
dc.titleNovel 3,4-disubstituted-Neu5Ac2en derivatives as probes to investigate flexibility of the influenza virus sialidase 150-loop
dc.typeJournal article
dc.type.descriptionC1 - Articles
dc.type.codeC - Journal Articles
gro.date.issued2013
gro.hasfulltextNo Full Text
gro.griffith.authorvon Itzstein, Mark
gro.griffith.authorThomson, Robin J.
gro.griffith.authorMaggioni, Andrea
gro.griffith.authorRudrawar, Santosh


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