Novel inhibitors of influenza sialidases related to zanamivir. Heterocyclic replacements of the glycerol sidechain

A series of substituted 4-amino-4H-pyran-2-carboxylic acid 6-triazoles and oxadiazoles are described. The compounds are inhibitors of influenza virus sialidases which, in general, show a similar pattern of activity and selectivity to recently reported 4H-pyran-2-carboxylic acid 6-carboxamides. Dihyd...

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Bibliographic Details
Published in:Bioorganic & medicinal chemistry letters 1997-09, Vol.7 (17), p.2239-2242
Main Authors: Smith, Paul W., Whittington, Andrew R., Sollis, Steven L., Howes, Peter D., Taylor, Neil R.
Format: Article
Language:English
Subjects:
Antibiotics. Antiinfectious agents. Antiparasitic agents
Antiviral agents
Biological and medical sciences
Medical sciences
Pharmacology. Drug treatments
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Summary:A series of substituted 4-amino-4H-pyran-2-carboxylic acid 6-triazoles and oxadiazoles are described. The compounds are inhibitors of influenza virus sialidases which, in general, show a similar pattern of activity and selectivity to recently reported 4H-pyran-2-carboxylic acid 6-carboxamides. Dihydropyran derivatives 4a-h have been prepared and evaluated as inhibitors of influenza virus sialidases. Compounds 4f and 4h are potent and selective inhibitors of influenza A sialidase.
ISSN:0960-894X
1464-3405
DOI:10.1016/S0960-894X(97)00399-5