Abstract
A series of acylguanidine-modified zanamivir analogs were synthesized and their inhibitory activities against the NAs of avian influenza viruses (H1N1 and H3N2) were evaluated. In particular, zanamivir derivative , with a hydrophobic naphthalene substituent, exhibits the best inhibitory activity against group-1 NA with an IC50 of 20 nM.
Publication types
-
Research Support, Non-U.S. Gov't
MeSH terms
-
Antiviral Agents / chemical synthesis
-
Antiviral Agents / chemistry
-
Antiviral Agents / pharmacology*
-
Dose-Response Relationship, Drug
-
Enzyme Inhibitors / chemical synthesis
-
Enzyme Inhibitors / chemistry
-
Enzyme Inhibitors / pharmacology*
-
Guanidine / analogs & derivatives*
-
Guanidine / chemistry
-
Guanidine / pharmacology*
-
Influenza A Virus, H1N1 Subtype / drug effects
-
Influenza A Virus, H3N2 Subtype / drug effects
-
Microbial Sensitivity Tests
-
Molecular Structure
-
Neuraminidase / antagonists & inhibitors*
-
Neuraminidase / metabolism
-
Structure-Activity Relationship
-
Zanamivir / analogs & derivatives*
-
Zanamivir / chemical synthesis
-
Zanamivir / chemistry
-
Zanamivir / pharmacology*
Substances
-
Antiviral Agents
-
Enzyme Inhibitors
-
Neuraminidase
-
Guanidine
-
Zanamivir