Syntheses of triazole-modified zanamivir analogues via click chemistry and anti-AIV activities

Article abstract of DOI:10.1016/j.bmcl.2006.07.047

Sixteen novel 4-triazole-modified zanamivir (1) analogues were synthesized using the click reactions, and their inhibitory activities against avian influenza virus (AIV, H5N1) were determined. Compound 3b exerts promising inhibitory activity with EC₅₀ of 6.4 μM, which is very close to that of zanamivir (EC₅₀ = 2.8 μM). Molecular modeling provided the information about the binding model between inhibitors and neuraminidase, which are in good agreement with inhibitory activities.