neuraminidase-in-1

Neuraminidase-IN-1 (Compound Y-1) is a novel neuraminidase inhibitor.

NDV-IN-1 is an antiviral agent with high neuraminidase inhibitory activity, demonstrating significant in vitro inhibitory effects against Newcastle disease virus (NDV). It effectively prevents NDV infection of Vero cells by inhibiting the release of virus particles from infected cells [1].

Neuraminidase-IN-16 (Compound 43b) serves as a potent inhibitor of neuraminidase, demonstrating IC50 values of 0.031, 0.15, 0.25, 0.60, 0.63, and 10.08 μM against neuraminidase from H5N1, H5N8, H1N1, H3N2, H5N1–H274Y, and H1N1–H274Y strains, respectively [1].

Neuraminidase-IN-13 (Compound 10), a neuraminidase inhibitor exhibiting antiviral activity, demonstrates significant inhibition of NDV infection in Vero cells with minimal cytotoxicity by impeding the release of viral particles from infected cells [1].

Neuraminidase-IN-17 (compound N10), characterized as a neuraminidase inhibitor, demonstrates an EC 50 of 0.11 μM and exhibits antiviral activity in vitro [1].

Neuraminidase-IN-18 (compound N5), a novel polyheterocyclic neuraminidase (NA) inhibitor, demonstrates significant inhibitory activity against H5N1 NA, with an IC 50 of 0.14 μM against the wild-type H5N1 NA and 0.27 μM against the H5N1-H274Y mutant NA. This compound effectively binds to NAs, inhibiting influenza virus replication at the cellular level [1].

Neuraminidase-IN-10 is a neuraminidase inhibitor that exhibits anti-influenza effects and is able to act on H1N1 (IC50: 2.6 nM), H5N1 (IC50: 5.1 nM) and H5N8 (IC50: 1.65 nM).

Neuraminidase-IN-11 (15e) is a selective and potent neuraminidase (NA) inhibitor, effective against the neuraminidase of H1N1 virus (IC50: 4.7 nM), H5N1 virus (IC50: 8.46 nM), and H5N8 virus (IC50: 1.5 nM).

Ganglioside GM1 asialo is a component of cellular lipid rafts and can be formed by the cleavage of the sialic acid residue from ganglioside GM1 by neuraminidase. Ganglioside GM1 asialo is a glycolipid receptor for P. aeruginosa flagellin and stimulates defensive responses in host cells, including extracellular ATP release, calcium mobilization, and ERK1/2 phosphorylation when stimulated by flagellin and an anti-ganglioside GM1 asialo antibody. The percentage of ganglioside GM1 asialo-positive natural killer (NK) and CD8+ T cells in lung is increased in a mouse model of respiratory syncytial virus (RSV) infection compared with healthy animals. Depletion of ganglioside GM1 asialo-positive NK and T cells reduces IFN-γ levels in the lung, reduces weight loss, and increases lung viral load in RSV-infected mice. Ganglioside GM1 asialo mixture contains ganglioside GM1 asialo molecular species with C18:1 and C20:1 sphingoid backbones.

Zanamivir-13C,15N2is intended for use as an internal standard for the quantification of zanamivir by GC- or LC-MS. Zanamivir is a sialic acid analog that inhibits neuraminidase release of newly replicated influenza virus particles.1It has been shown to selectively inhibit the growth of influenza A and B viruses in plaque reduction assays with IC50values ranging from 5 to 14 nM and to directly inhibit influenza A and B virus neuraminidases with IC50values ranging from 0.6 to 7.9 nMin vitro. Intranasal zanamivir administration at 0.4 mg/kg twice daily reduces mortality and viral titers in lung homogenates of mice infected with influenza. 1.Elliott, M.Zanamivir: From drug design to the clinicPhilos. Trans. R. Soc. Lond. B Biol Sci.356(1416)1885-1893(2001)

Oseltamivir acid methyl ester is a precursor form of oseltamivir acid, which is converted to oseltamivir acid by carboxylesterase 1 (CES1). Oseltamivir acid, in turn, acts as a neuraminidase inhibitor and antiviral agent [1].

Neuraminidase-IN-6 (Compound 5c), a derivative of 1,3,4-triazole-3-acetamide, is a potent neuraminidase inhibitor with an IC50 value of 0.11 μM, making neuraminidase (NA) an ideal target for anti-influenza drug development [1].

Neuraminidase-IN-5 (Compound 5b), a dihydrofurocoumarin derivative, acts as a potent neuraminidase (NA) inhibitor, exhibiting significant inhibition with an IC 50 of 0.02 μM. Given NA's role in influenza pathogenesis, this compound emerges as a promising candidate for anti-influenza drug development [1].

Neuraminidase-IN-8 (Compound 6d) is a potent neuraminidase inhibitor with a low IC50 of 0.027 μM, demonstrating significant anti-influenza activities [1].

Influenza A virus-IN-4 (compound 23b), a derivative of Oseltamivir, is a highly effective neuraminidase inhibitor that exerts potent inhibitory effects on influenza viruses [1].

3,5-O-Dicaffeoylquinic acid (Isochlorogenic Acid A) is an isolated compound from Artemisia argyi; its ester derivatives exert anti-leucyl-tRNA synthetase of Giardia lamblia (GlLeuRS) and potential anti-giardial effects. 3,5-O-Dicaffeoylquinic acid (Isochlorogenic Acid A) as a neuraminidase inhibitory ligand in Flos Lonicerae, it has neuroprotective effects on SH-SY5Y cells and senescence-accelerated-prone mice 8 through the up-regulation of phosphoglycerate kinase-1. 3,5-O-Dicaffeoylquinic acid (Isochlorogenic Acid A) also has antioxidant and anti-complementary activities.

The binding affinities of ganoderic acid DM andGanoderic acid ζ (ΔGbind, -16.83 and-10.99 kcal mol-1) are comparable to that of current commercial drug oseltamivir (-23.62 kcal mol-1);Ganoderic acid DM is a potential source of anti-influenza ingredient, with novel binding pattern and advantage over oseltamivir, it has steric hindrance on the 150 cavity of N1 protein, and exerts activities across the H274Y and N294S mutations, is the attractive candidates of novel neuraminidase (NA) inhibitors.Ganoderic acid zeta has cytotoxicity in vitro against Meth-A and LLC cell lines.