Synthesis and influenza virus sialidase inhibitory activity of analogues of 4-Guanidino-Neu5Ac2en (Zanamivir) modified in the glycerol side-chain
| Autor: | Paul S. Jones, Steven P Keeling, Stephen Swanson, David Cedric Humber, Paul F Martin, Peter C. Cherry, David M. Andrews, Caroline D Shaw |
|---|---|
| Rok vydání: | 2001 |
| Předmět: |
Glycerol
Stereochemistry medicine.drug_class Orthomyxoviridae Neuraminidase Carboxamide Viral Plaque Assay Sialidase Crystallography X-Ray Chemical synthesis Antiviral Agents Guanidines Virus chemistry.chemical_compound Zanamivir Drug Discovery medicine Humans Enzyme Inhibitors Pyrans Pharmacology biology Chemistry Organic Chemistry General Medicine biology.organism_classification Influenza B virus Enzyme inhibitor Influenza A virus Aldonic acid biology.protein Sialic Acids medicine.drug |
| Zdroj: | European journal of medicinal chemistry. 34(7-8) |
| ISSN: | 0223-5234 |
| Popis: | Analogues of 4-Guanidino-Neu5Ac2en (Zanamivir) have been prepared containing carbamate substituents at the 7-hydroxy position. (4S,5R,6R)-5-Acetylamino-6-{1R-[(6-aminohexyl)carbamoyloxy]-2R,3-dihydroxypropyl}-4-guanidino-5,6-dihydro-4H-pyran-2carboxylic acid and (4S,5R,6R)-5-Acetylamino-6-{1R-[heptylcarbamoyloxy]-2R,3-dihydroxypropyl}-4-guanidino-5,6-dihydro4H-pyran2-carboxylic acid were the two analogues possessing activity comparable to Zanamivir, showing potent inhibition of influenza virus sialidases and good antiviral activity in vitro. |
| Databáze: | OpenAIRE |
| Externí odkaz: |
|
Full Text from ScienceDirect