Synthesis and activity of C2-substituted analogs of influenza neuraminidase inhibitor GS 4071

Article abstract of DOI:10.1016/S0960-894X(97)00331-4

The influence of C₂-substitution of GS 4071 on the influenza neuraminidase inhibitory activity was investigated. The introduction of lipophilic substituents (chloro, methyl, and methylthio) at the C₂ position resulted in a significant decrease of the activity. This result indicates that at the enzyme active site there is limited hydrophobic pocket for a group at the C₂ position of GS 4071.