| Table 1: Chemical structures of compounds 5–14 and their inhibitory activities against sialidase of three different strains of influenza A virus (A/PR/8/34 virus [H1N1], A/Memphis/1/71 virus [H3N2], and A/Duck/313/78 virus [H5N3]). |
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Viral sialidase inhibition (IC50, μM)a | Human sialidase inhibition (IC50, μM)a | | R | H1N1 | H3N2 | H5N3 | NEU1 | NEU2 | NEU3 | NEU4 |
| | 2 | DANA | 1 | 9 | 11 | 143 | 43 | 61 | 74 | | 5 | Methyl | 22 | 34 | 97 | 58 | >1000 | >1000 | 580 | | 6 | Phenyl | >1000 | >1000 | >1000 | — | — | — | — | | 7 | Cyclopentyl | 850 | >1000 | >1000 | — | — | — | — | | 8 | Cyclopropyl | 9 | 16 | 98 | 680 | >1000 | >1000 | 825 | | 9 | Propyl | 97 | 559 | >1000 | — | — | — | — | | 10 | 2-Methylpropyl | 59 | >1000 | >1000 | — | — | — | — | | 11 | Isopropyl | 54 | 680 | >1000 | — | — | — | — | | 12 | n-Butyl | 34 | 159 | >1000 | — | — | — | — | | 13 | tert-Butyl | 78 | 770 | >1000 | — | — | — | — | | 14 | 2-Ethylpropyl | 698 | >1000 | >1000 | — | — | — | — |
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aIC50 values of human sialidases are citied from [39].
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