The synthesis and biological evaluation of lactose-based sialylmimetics as inhibitors of rotaviral infection

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Title The synthesis and biological evaluation of lactose-based sialylmimetics as inhibitors of rotaviral infection
Author Liakatos, Angela; Kiefel, Milton; Fleming, Fiona; Coulson, Barbara; von Itzstein, Mark
Journal Name Bioorganic & Medicinal Chemistry
Year Published 2006
Place of publication Oxford, UK
Publisher Pergamon Press
Abstract Rotaviruses are the most significant cause of gastroenteritis in young children and are responsible for over 600,000 infant deaths annually. The rotaviral haemagglutinin protein (VP8*) of some strains has been implicated in early recognition and binding events of host cell-surface sialoglycoconjugates, and is therefore an attractive target for potential therapeutic intervention. Since N-acetylneuraminic acid α(2,3)-linked to galactose is believed to be the minimum binding epitope of rotavirus to host cells, we report here our development of an efficient and flexible synthetic route to a range of lactose-based sialylmimetics of α(2,3)-linked thiosialosides. These compounds were biologically evaluated as inhibitors of rotaviral infection using an in vitro neutralisation assay. The results suggest that these lactose-based sialylmimetics are not inhibitors of the rhesus rotavirus strain; however, they do exhibit modest inhibition of the human (Wa) strain, presumably through inhibition of the rotaviral adhesion process.
Peer Reviewed Yes
Published Yes
Publisher URI http://www.elsevier.com/wps/find/journaldescription.cws_home/129/description#description
Alternative URI http://dx.doi.org/10.1016/j.bmc.2005.08.057
Volume 14
Page from 739
Page to 757
ISSN 0968-0896
Date Accessioned 2007-02-23
Date Available 2009-10-19T05:23:02Z
Language en_AU
Research Centre Institute for Glycomics
Faculty Institute for Glycomics
Subject PRE2009-Biological and Medical Chemistry; PRE2009-Organic Chemical Synthesis
URI http://hdl.handle.net/10072/13716
Publication Type Journal Articles (Refereed Article)
Publication Type Code c1

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