Cyclopentane Neuraminidase Inhibitors With Potent In Vitro Anti-Influenza Virus Activities

Document Type

Article

Journal/Book Title/Conference

Cyclopentane neuraminidase inhibitors with potent in vitro anti-influenza virus activities

Volume

45

Publication Date

2001

First Page

743

Last Page

748

Abstract

A novel series of cyclopentane derivatives have been found to exhibit potent and selective inhibitory effects on influenza virus neuraminidase. These compounds, designated RWJ-270201, BCX-1827, BCX-1898, and BCX-1923, were tested in parallel with zanamivir and oseltamivir carboxylate against a spectrum of influenza A (H1N1, H3N2, and H5N1) and influenza B viruses in MDCK cells. Inhibition of viral cytopathic effect ascertained visually and by neutral red dye uptake was used, with 50% effective (virus-inhibitory) concentrations (EC50) determined. Against the H1N1 viruses A/Bayern/07/95, A/Beijing/262/95, A/PR/8/34, and A/Texas/36/91, EC50s (determined by neutral red assay) of the novel compounds were ≤1.5 μM. Twelve strains of H3N2 and two strains of avian H5N1 viruses were inhibited at

Comments

Antimicrob Agents Chemother. 45:743-748. PMID: 11181354

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