Highly potent and long-acting trimeric and tetrameric inhibitors of influenza virus neuraminidase
- Resource Type
- Authors
- Simon J. F. Macdonald; David Gower; Andrew M. Mason; Stephanie Hamilton; Betty Jin; Guy Y. Krippner; Rob J. Fenton; Van N.B. Nguyen; Angela Luttick; Keith G. Watson; Simon P. Tucker; Rachel Cameron; Darryl Mcconnell; Wen-Yang Wu
- Source
- Bioorganic & Medicinal Chemistry Letters. 14:1589-1592
- Subject
- medicine.drug_class
Stereochemistry
viruses
Clinical Biochemistry
Orthomyxoviridae
Neuraminidase
Pharmaceutical Science
Antiviral Agents
Guanidines
Biochemistry
Virus
Mice
Zanamivir
Orthomyxoviridae Infections
Drug Discovery
medicine
Animals
Enzyme Inhibitors
Molecular Biology
Pyrans
chemistry.chemical_classification
Infectivity
biology
Neuraminidase inhibitor
Chemistry
Organic Chemistry
virus diseases
biochemical phenomena, metabolism, and nutrition
biology.organism_classification
Virology
respiratory tract diseases
Enzyme
Influenza A virus
Enzyme inhibitor
Sialic Acids
biology.protein
Molecular Medicine
medicine.drug
- Language
- ISSN
- 0960-894X
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.