tetano
Editor, Senior Moderator
Bioorg Med Chem. 2013 Jun 6. pii: S0968-0896(13)00503-8. doi: 10.1016/j.bmc.2013.05.054. [Epub ahead of print]
Novel 3,4-disubstituted-Neu5Ac2en derivatives as probes to investigate flexibility of the influenza virus sialidase 150-loop.
Rudrawar S, Dyason JC, Maggioni A, Thomson RJ, Itzstein MV.
Source
Institute for Glycomics, Griffith University, Gold Coast Campus, Queensland 4222, Australia.
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.
Copyright ? 2013 Elsevier Ltd. All rights reserved.
PMID:
23800724
[PubMed - as supplied by publisher]
http://www.ncbi.nlm.nih.gov/pubmed/23800724
Novel 3,4-disubstituted-Neu5Ac2en derivatives as probes to investigate flexibility of the influenza virus sialidase 150-loop.
Rudrawar S, Dyason JC, Maggioni A, Thomson RJ, Itzstein MV.
Source
Institute for Glycomics, Griffith University, Gold Coast Campus, Queensland 4222, Australia.
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.
Copyright ? 2013 Elsevier Ltd. All rights reserved.
PMID:
23800724
[PubMed - as supplied by publisher]
http://www.ncbi.nlm.nih.gov/pubmed/23800724