Table 1.
Anti‐influenza virus activity and cytotoxicity in MDCK a cell cultures.
| Compound | Antiviral EC50 b | ||||||||
|---|---|---|---|---|---|---|---|---|---|
| A/H1N1 | A/H3N2 | IBV | Cytotoxicity | ||||||
| CPE | MTS | CPE | MTS | CPE | MTS | MCCc | CC50 d | ||
| All values in µM | |||||||||
| 1a | H | > 100 | > 100 | > 100 | > 100 | > 100 | > 100 | 100 | > 100 |
| 1b | 7‐Me | > 100 | > 100 | > 100 | > 100 | > 100 | > 100 | 20 | 11 |
| 1c | 8‐Me | > 100 | > 100 | > 100 | > 100 | > 100 | > 100 | > 100 | > 100 |
| 1d | 8‐Et | > 100 | > 100 | > 100 | > 100 | > 100 | > 100 | > 100 | > 100 |
| 1e | 8‐Pr | > 100 | > 100 | > 100 | > 100 | > 100 | > 100 | 100 | > 100 |
| 1f | 8‐t‐Bu | > 100 | > 100 | > 100 | > 100 | > 100 | > 100 | > 100 | > 100 |
| 2a | H | > 100 | > 100 | > 100 | > 100 | > 100 | > 100 | ≥ 20 | 92 |
| 2b | 7‐Me | > 100 | > 100 | > 100 | > 100 | > 100 | > 100 | ≥ 20 | 78 |
| 2c | 8‐Me | > 100 | > 100 | 2.4 ± 0.8 | 1.3 ± 0.3 | > 100 | > 100 | ≥ 20 | 39 ± 25 |
| 2d | 8‐Et | > 100 | > 100 | > 100 | > 100 | > 100 | > 100 | 20 | 13 |
| 2e | 8‐Pr | > 100 | > 100 | > 100 | > 100 | > 100 | > 100 | 4.0 | 14 |
| 2f | 8‐t‐Bu | > 100 | > 100 | > 100 | > 100 | > 100 | > 100 | ≥ 20 | > 100 |
| Oseltamivir carboxylate | 0.5 | 0.4 | 0.8 | 0.4 | 0.8 | 0.6 | > 100 | > 100 | |
| Ribavirin | 8.9 | 7.1 | 6.8 | 1.3 | 9.0 | 5.3 | > 100 | > 100 | |
| Rimantadine | 8.0 | 8.7 | 0.7 | 0.8 | > 200 | > 200 | > 200 | > 200 | |
a
Madin Darby canine kidney cells.
b
Compound concentration producing 50% inhibition of virus‐induced cytopathic effect, as determined by visual scoring of the CPE, or by the MTS cell viability assay. Virus strains: A/Ned/378/05 (A/H1N1); A/HK/7/87 (A/H3N2): B/Ned/537/05 (IBV).
c
Minimum compound concentration that causes a microscopically detectable alteration of normal cell morphology.
d
50% cytotoxic concentration based on the MTS cell viability assay.