1. Highly potent and long-acting trimeric and tetrameric inhibitors of influenza virus neuraminidase.
- Author
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Watson KG, Cameron R, Fenton RJ, Gower D, Hamilton S, Jin B, Krippner GY, Luttick A, McConnell D, MacDonald SJ, Mason AM, Nguyen V, Tucker SP, and Wu WY
- Subjects
- Animals, Antiviral Agents pharmacology, Antiviral Agents therapeutic use, Enzyme Inhibitors pharmacology, Enzyme Inhibitors therapeutic use, Guanidines, Influenza A virus drug effects, Mice, Neuraminidase metabolism, Orthomyxoviridae Infections drug therapy, Orthomyxoviridae Infections enzymology, Pyrans, Sialic Acids chemistry, Sialic Acids pharmacology, Sialic Acids therapeutic use, Zanamivir, Antiviral Agents chemistry, Enzyme Inhibitors chemistry, Influenza A virus enzymology, Neuraminidase antagonists & inhibitors
- Abstract
A set of trimeric and tetrameric derivatives 6-11 of the influenza virus neuraminidase inhibitor zanamivir 1 have been synthesized by coupling a common monomeric zanamivir derivative 3 onto various multimeric carboxylic acid core groups. These discrete multimeric compounds are all significantly more antiviral than zanamivir and also show outstanding long-lasting protective activity when tested in mouse influenza infectivity experiments.
- Published
- 2004
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