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

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

Source and publish data:

Bioorganic and Medicinal Chemistry Letters p. 1847 - 1850 (1997)

Update date:2022-07-30

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Authors:

Zhang, Lijun

Williams, Matthew A.

Mendel, Dirk B.

Escarpe, Paul A.

Kim, Choung U.

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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.

Full text of DOI:10.1016/S0960-894X(97)00331-4

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