Sialidase inhibitors related to zanamivir: Synthesis and biological evaluation of 4H-pyran 6-ether and ketone

Synthesis of 5R-Acetamido-4S-amino-4H-pyran-6R-O-(1-ethyl)propyl and 6R-(1-oxo-2-ethyl)butyl 2-carboxylic acids ( 4 and 5) and their evaluation as inhibitors of influenza virus sialidase is described. Both compounds showed good inhibitory activity with marked selectivity for influenza A sialidase. T...

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Bibliographic Details
Published in:Bioorganic & medicinal chemistry letters 1999-02, Vol.9 (4), p.601-604
Main Authors: Smith, Paul W., Robinson, J.Ed, Evans, Derek N., Sollis, Steven L., Howes, Peter D., Trivedi, Naimisha, Bethell, Richard C.
Format: Article
Language:English
Subjects:
Antibiotics. Antiinfectious agents. Antiparasitic agents
Antiviral agents
Biological and medical sciences
Enzyme Inhibitors - chemistry
Enzyme Inhibitors - pharmacology
Guanidines
Ketones - chemistry
Ketones - pharmacology
Medical sciences
Neuraminidase - antagonists & inhibitors
Pharmacology. Drug treatments
Pyrans - chemistry
Pyrans - pharmacology
Sialic Acids - chemistry
Sialic Acids - pharmacology
Zanamivir
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Summary:Synthesis of 5R-Acetamido-4S-amino-4H-pyran-6R-O-(1-ethyl)propyl and 6R-(1-oxo-2-ethyl)butyl 2-carboxylic acids ( 4 and 5) and their evaluation as inhibitors of influenza virus sialidase is described. Both compounds showed good inhibitory activity with marked selectivity for influenza A sialidase. The synthesis and influenza virus sialidase inhibitory activity of 4 and 5 is described. Both compounds are selective inhibitors of influenza A sialidase
ISSN:0960-894X
1464-3405
DOI:10.1016/S0960-894X(99)00031-1