Chanmei Lv, Fangyuan Shi
May 17, 2022
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Journal
Letters in Drug Design & Discovery
Abstract
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. All compounds were synthesized in good yields starting from commercially available 2-(4-aminophenyl) acetic acid using a suitable synthetic strategy. These compounds showed potent inhibitory activity against influenza A NA. Several compounds with alkylated amino group showed moderate NA subtype selectivity, among which (7i) displayed the best. (7i) activity against H5N1 was more than 10 times better than H9N2, and could be used as lead compounds in the future.