1P13: k) Synthesis and anti-influenza virus activity of 4-guanidino-7-substituted neu5Ac2en derivatives

T. Honda et al.⁴⁵ synthesized a series of Zanamivir derivative possessing C-7 substituted glycerol side chains using enzyme-catalyzed aldol condensation as shown in scheme 13 (d and e) and evaluated in vitro inhibitory activity against influenza A virus sialidase. Furthermore, replacement of the C-7 hydroxyl group of zanamivir by small lipophilic substituents (F, OMe, OEt, N₃) improved influenza A virus plaque reduction activity.

____________________
45. T. Honda, T. Masuda, S. Yoshida, M. Arai, Y. Kobayashi, and M. Yamashita, Bioorg. Med. Chem. Lett., 2000, 12, 1921.
Next Page