Synthesis and anti-influenza virus activity of 4-guanidino-7-substituted Neu5Ac2en derivatives.
Honda T, Masuda T, Yoshida S, Arai M, Kobayashi Y, Yamashita M.
Substitution of 7-OH by small hydrophobic groups on zanamivir resulted in the retaining of low nanomolar inhibitory activities against not only influenza A virus sialidase but also influenza A virus in cell culture. These compounds were prepared by treatment of the corresponding 7-substituted sialic acids derived from 4-modified N-acetyl-D-mannosamine (ManNAc) using enzyme-catalyzed aldol condensation.