Key result
Compound 8a demonstrated high antiviral activity against influenza A H3N2 and H1N1 (IC50 = 7.41 and 5.63 μm, respectively) with low cytotoxicity (TC50 > 200 μm) in vitro.
Effect estimate: IC50 = 7.41, 5.63 μm for H3N2 and H1N1; TC50 > 200 μm
Compound 8a is a novel nucleoside analogue with potent in vitro activity against influenza A viruses and low cytotoxicity, representing a potential candidate for further development.
Does not support clinical use; leaves open further preclinical development of 8a for influenza A.
Novel 2-oxo-pyrazine-3-carboxamide-yl nucleoside analogues and their epimers were designed, synthesized and evaluated for their activities against influenza A viruses H1N1 and H3N2 in Madin-Darby canine kidney cells. All the compounds showed low cytotoxicities in these anti-influenza tests. One of the epimers, 4-[(1S, 3R, 4R, 7R)-7-hydroxy-1-(hydroxymethyl)-2,5-dioxabicyclo[2.2.1]heptan-3-yl]-3-oxo-3,4-dihydropyrazine-2-carboxamide 8a, with high antiviral activities (IC50 = 7.41, 5.63 μm for H3N2 and H1N1, respectively) and remarkable low cytotoxicity (TC50 > 200 μm), has great potential for further development as a novel anti-influenza A agent. Molecular docking of compound 8a with RNA-dependent RNA polymerase was performed to understand the binding mode between these inhibitors and the active site of RdRp and to rationalize some SARs.
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Gao et al. (2014) studied Influenza A viruses H1N1 and H3N2. 2-oxo-pyrazine-3-carboxamide-yl nucleoside analogues (compound 8a) was evaluated on Antiviral activity (IC50) and cytotoxicity (TC50) (IC50 = 7.41, 5.63 μm for H3N2 and H1N1; TC50 > 200 μm). Compound 8a demonstrated high antiviral activity against influenza A H3N2 and H1N1 (IC50 = 7.41 and 5.63 μm, respectively) with low cytotoxicity (TC50 > 200 μm) in vitro.
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