- Structure-activity relationships of carbocyclic influenza neuraminidase inhibitors
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The structure-activity relationships (SAR) for a new class of potent inhibitors (1) of influenza neuraminidase are described. Systematic modifications of substituents at the C-3, C-4, and C-5 positions of the carbocyclic ring were performed to establish fundamental SAR to assist in the design of potent inhibitors with activity against both of influenza A and B viruses.
- Williams, Matthew A.,Lew, Willard,Mendel, Dirk B.,Tai, Chun Y.,Escarpe, Paul A.,Laver, W. Graeme,Stevens, Raymond C.,Kim, Choung U.
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- Novel compound, its synthetic method and therapeutic use (by machine translation)
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Novel compounds are described. The compounds generally comprise an acidic group, a basic group, a substituted amino or N-acyl and a group having an optionally hydroxylated alkane moiety. Pharmaceutical compositions comprising the inhibitors of the invention are also described. Methods of inhibiting neuraminidase in samples suspected of containing neuraminidase are also described. Antigenic materials, polymers, antibodies, conjugates of the compounds of the invention with labels, and assay methods for detecting neuraminidase activity are also described.
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