dc.contributor.author | Rudrawar, Santosh | |
dc.contributor.author | Dyason, Jeffrey C | |
dc.contributor.author | Maggioni, Andrea | |
dc.contributor.author | Thomson, Robin J | |
dc.contributor.author | von Itzstein, Mark | |
dc.date.accessioned | 2017-05-03T16:05:46Z | |
dc.date.available | 2017-05-03T16:05:46Z | |
dc.date.issued | 2013 | |
dc.date.modified | 2014-03-27T03:59:49Z | |
dc.identifier.issn | 0968-0896 | |
dc.identifier.doi | 10.1016/j.bmc.2013.05.054 | |
dc.identifier.uri | http://hdl.handle.net/10072/57319 | |
dc.description.abstract | Novel 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.peerreviewed | Yes | |
dc.description.publicationstatus | Yes | |
dc.language | English | |
dc.language.iso | eng | |
dc.publisher | Pergamon | |
dc.publisher.place | United Kingdom | |
dc.relation.ispartofstudentpublication | N | |
dc.relation.ispartofpagefrom | 4820 | |
dc.relation.ispartofpageto | 4830 | |
dc.relation.ispartofissue | 16 | |
dc.relation.ispartofjournal | Bioorganic Medicinal Chemistry | |
dc.relation.ispartofvolume | 21 | |
dc.rights.retention | Y | |
dc.subject.fieldofresearch | Medicinal and biomolecular chemistry | |
dc.subject.fieldofresearch | Biologically active molecules | |
dc.subject.fieldofresearch | Organic chemistry | |
dc.subject.fieldofresearch | Pharmacology and pharmaceutical sciences | |
dc.subject.fieldofresearch | Biochemistry and cell biology | |
dc.subject.fieldofresearchcode | 3404 | |
dc.subject.fieldofresearchcode | 340401 | |
dc.subject.fieldofresearchcode | 3405 | |
dc.subject.fieldofresearchcode | 3214 | |
dc.subject.fieldofresearchcode | 3101 | |
dc.title | Novel 3,4-disubstituted-Neu5Ac2en derivatives as probes to investigate flexibility of the influenza virus sialidase 150-loop | |
dc.type | Journal article | |
dc.type.description | C1 - Articles | |
dc.type.code | C - Journal Articles | |
gro.date.issued | 2013 | |
gro.hasfulltext | No Full Text | |
gro.griffith.author | von Itzstein, Mark | |
gro.griffith.author | Thomson, Robin J. | |
gro.griffith.author | Maggioni, Andrea | |
gro.griffith.author | Rudrawar, Santosh | |