Unsaturated N -acetyl- D-glucosaminuronic acid glycosides as inhibitors of influenza virus sialidase
Identifieur interne : 001737 ( Istex/Checkpoint ); précédent : 001736; suivant : 001738Unsaturated N -acetyl- D-glucosaminuronic acid glycosides as inhibitors of influenza virus sialidase
Auteurs : Maretta C. Mann [Australie] ; Tasneem Islam [Australie] ; Jeffrey C. Dyason [Australie] ; Pas Florio [Australie] ; Carolyn J. Trower [Australie] ; Robin J. Thomson [Australie] ; Mark Von Itzstein [Australie]Source :
- Glycoconjugate Journal [ 0282-0080 ] ; 2006.
Abstract
Abstract: The threat of pandemic influenza is a significant concern of governments worldwide. There is a very limited and relatively expensive armament to tackle such a pandemic should it occur. This fact provides much impetus to the scientific community for the discovery of new and less expensive anti-influenza drugs. Our longstanding interest in the inhibition of influenza virus sialidase, coupled with the development of simple carbohydrates that mimic an unsaturated derivative of the enzyme's naturally-occurring ligand, N-acetylneuraminic acid, has led us to investigate the development of influenza virus sialidase inhibitors based on these mimetics. We have successfully prepared a range of these compounds, in good yield, from the relatively inexpensive carbohydrate N-acetylglucosamine utilising a short synthetic procedure. We have employed a sialidase inhibition assay for biological evaluation of the target compounds and to our delight these mimetics have displayed significant inhibition of influenza virus sialidase.
Url:
DOI: 10.1007/s10719-006-5445-9
Affiliations:
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-acetyl- D-glucosaminuronic acid glycosides as inhibitors of influenza virus sialidase</title>
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<front><div type="abstract" xml:lang="en">Abstract: The threat of pandemic influenza is a significant concern of governments worldwide. There is a very limited and relatively expensive armament to tackle such a pandemic should it occur. This fact provides much impetus to the scientific community for the discovery of new and less expensive anti-influenza drugs. Our longstanding interest in the inhibition of influenza virus sialidase, coupled with the development of simple carbohydrates that mimic an unsaturated derivative of the enzyme's naturally-occurring ligand, N-acetylneuraminic acid, has led us to investigate the development of influenza virus sialidase inhibitors based on these mimetics. We have successfully prepared a range of these compounds, in good yield, from the relatively inexpensive carbohydrate N-acetylglucosamine utilising a short synthetic procedure. We have employed a sialidase inhibition assay for biological evaluation of the target compounds and to our delight these mimetics have displayed significant inhibition of influenza virus sialidase.</div>
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