Table 2.
Inhibition Constants (Ki) of Viral Neuraminidases by Small-Molecule (2) and Polymeric (4) Zanamivir Derivatives Against Both Wild-Type and Drug-Resistant Human and Avian Influenza Strains
|
Ki (nM of Zanamivira) |
||
|---|---|---|
| Strain | 2 | 4 |
| A/Wuhan/359/95 | 3.1 ± 1.0 | 0.93 ± 0.12 |
| A/Wuhan/359/95 E119V | 1.9 ± 0.8 | 0.90 ± 0.10 |
| A/turkey/MN/833/80 | 4.6 ± 0.9 | 0.27 ± 0.16 |
| A/turkey/MN/833/80 E119D | 800 ± 150 | 0.37 ± 0.12 |
| A/turkey/MN/833/80 E119G | 370 ± 20 | 0.13 ± 0.05 |
a
All values were determined from experiments run at least in triplicate unless otherwise indicated. The Ki values are expressed in concentrations of zanamavir, whether free or conjugated to poly-L-glutamine. For other conditions, see the Materials and Methods section.