Abstract
Introduction: A series of hydrophobic phenylacetic acid derivatives introducing an aromatic lipophilic side chain at C-3 amino and an acetyl or isopropionyl at C-4 amino were synthesized and evaluated for their ability to inhibit neuraminidase (NA) of influenza A virus.
Methods: All compounds were synthesized in good yields starting from commercially available 2-(4- aminophenyl) acetic acid using a suitable synthetic strategy.
Results: These compounds showed potent inhibitory activity against influenza A NA. Several compounds with alkylated amino group showed moderate NA subtype selectivity, among which compound (7i) displayed the best.
Conclusion: Compound (7i) activity against H5N1 was more than 10 times better than H9N2, and could be used as lead compounds in the future.
Keywords: Influenza virus, neuraminidase, phenylacetic acid, inhibitors, rational drug design, structure-activity.
Graphical Abstract
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