Influenza A virus-IN-6 (compound 16j) is a potent and selective influenza A virus inhibitor with an IC50 of 3.88 µM and CC50 of 36.64 µM. Influenza A virus-IN-6 shows anti-IAV activity with low cytotoxicity[1].
Influenza virus-IN-7 (Example 16) is an orally active cap-dependent endonuclease inhibitor that can be used for the research of influenza viral infectious diseases[1].
NS1-IN-1 (compound 3) is a potent NS1 inhibitor. NS1 is a major influenza A virus virulence factor that inhibits host gene expression. NS1-IN-1 decreases viral protein levels, contributing to the reduction of virus replication. NS1-IN-1 shows antiviral activity by repressing the activity of mTORC1 in a TSC1-TSC2-dependent manner[1].
Diphyllin is an arylnaphthalene lignan isolated from Justicia procumbens and is a potent HIV-1 inhibitor with an IC50 of 0.38 μM. Diphyllin is active against vesicular stomatitis virus (VSV) and influenza virus[1]. Diphyllin is a vacuolar type H+-ATPase (V-ATPase) inhibitor with an IC50 value of 17 nM and inhibits lysosomal acidification in human osteoclasts[2]. Diphyllin inhibits NO production with an IC50 of 50 μM and has anticancer and anti-inflammatory activities[3].
JNJ4796 is an oral active fusion inhibitor of influenza virus, neutralizing influenza A group 1 viruses by inhibiting hemagglutinin (HA)-mediated fusion. JNJ4796 mimics the functionality of the broadly neutralizing antibodies (bnAbs)[1].
Nucleozin targets influenza A nucleoprotein (NP), a multifunctional, RNA-binding protein necessary for virus replication. IC50 Value: Target: Influenza Virus NPNucleozin targets influenza A nucleoprotein, a multifunctional, RNA-binding protein necessary for virus replication. It induces the formation of nucleoptotein aggregates and inhibits its accumulation, interfering with viral replication. EC50 is in the nM range. Nucleozin is effective in H1N1, H3N2, and H5N1 flu virus strains.
Rimantadine-d4 hydrochloride is the deuterium labeled Rimantadine hydrochloride. Rimantadine hydrochloride is an anti-influenza virus agent[1][2].
Cap-dependent endonuclease-IN-26 is a cap-dependent endonuclease (CEN) inhibitor with an IC50 of 286 nM. Cap-dependent endonuclease-IN-26 shows antiviral activity against many influenza A and B strains[1].
Pimodivir (VX-787) is an orally bioavailable inhibitor of influenza A virus polymerases through interaction with the viral PB2 subunit.
Trimethoprim hydrochloride is a bacteriostatic antibiotic and an orally active dihydrofolate reductase inhibitor. Trimethoprim hydrochloride is active against a wide range of Gram-positive and Gram-negative aerobic bacteria. Trimethoprim hydrochloride has the potential for the research of urinary tract infections, Shigellosis and Pneumocystis pneumonia. Trimethoprim hydrochloride can inhibit infection of Influenza A virus in chick embryo when combinated with zinc[1][2][3][4].
Theaflavin is a suitable natural inhibitor against influenza A (H1N1) neuraminidase.
A-315675 is a potent highly potent inhibitor of A and B strain influenza virus neuraminidases inhibitor[1].
Cap-dependent endonuclease-IN-7 is a potent inhibitor of cap-dependent endonuclease (CEN). Cap-dependent endonuclease-IN-7 Inhibits the synthesis of viral mRNA and eventually inhibits virus proliferation. Cap-dependent endonuclease-IN-7 has the potential for the research of viral infections (including influenza A, influenza B and influenza C) (extracted from patent WO2020177715A1, compound 5)[1]
Zanamivir–cholesterol conjugate is a long-acting neuraminidase inhibitor with potent efficacy against drug-resistant influenza viruses.
Trifluoromethyl-tubercidin (TFMT) inhibits host MTr1 and suppresses virus replication. TFMT inhibits MTr1 through interaction at its S-adenosyl-l-methionine binding pocket to restrict influenza virus replication. TFMT was effective in inhibiting viral replication in mice, displayed little toxicity.
HSP90-IN-14 (compound 4) is a potent Hsp90 (heat shock protein 90) inhibitor, with a Kd of 0.26 μM. HSP90-IN-14 shows anti-influenza virus activity in MDCK cells, with EC50 values of 2.6, 3.9, and 17 μM for influenza A/H3N2, A/H1N1, and B, respectively[1].
Tetrahydroepiberberine is a isoquinoline alkaloid isolated from Corydalis impatiens (Pall). Tetrahydroepiberberine has antifungal and selective inhibition against the PI-3 virus activities[1].
Amitivir (LY 217896), a thiadiazole derivative, possesses broad antiviral activity against orthomyxo- and paramyxoviruses. Amitivir is effective against influenza A and B viruses[1][2].
4-O-Methylepisappanol (compound 9) is nature product that could be isolated from heartwood of Caesalpinia sappan. 4-O-Methylepisappanol is a potent neuraminidase inhibitor on the surface of influenza viruses with IC50 values of 42.8, 63.2, and 63.2 µM for A/Chicken/Korea/MS96/96 [H9N2], A/PR/8/34 [H1N1], and A/Hong Kong/8/68 [H3N2], respectively[1].
N-Acetylneuraminic acid-d3 is the deuterium labeled N-Acetylneuraminic acid.
M2e, human, consisting of the 23 extracellular residues of M2 (the third integral membrane protein of influenza A), has been remarkably conserved in all human influenza A, which is a valid and versatile vaccine candidate to protect against any strain of human influenza A[1].
Nepasaikosaponin K is an anti-influenza agent. Nepasaikosaponin K shows an EC50 of 17.91 μM against influenza virus A/WSN/33 (H1N1) in 239T-Gluc cells[1].
Benzimidazole is a heterocyclic aromatic organic compound and acts as an important pharmacophore in medicinal chemistry. Benzimidazole derivatives have been reported to possess various biological activities such as anti-cancer, anti-viral, anti-bacterial, anti-fungal, anti-helmintic, anti-inflammatory, proton pump inhibitor and anti-coagulant property[1][2][3].
ML303 is a pyrazolopyridine influenza virus nonstructural protein 1 (NS1) antagonist (IC90 = 155 nM), with an EC50 of 0.7 μM for Influenza A virus H1N1[1].
Arbidol (Umifenovir) hydrochloride is an broad-spectrum antiviral chemical agent which can inhibit cell entry of enveloped viruses by blocking viral fusion with host cell membraneIC50 value:Target: Antiviral; Anti-influenza agentin vitro: Arbidol was found to present potent inhibitory activity against enveloped and non-enveloped RNA viruses, including FLU-A, RSV, HRV 14 and CVB3 when added before, during, or after viral infection, with 50% inhibitory concentration (IC50) ranging from 2.7 to 13.8 microg/ml.However, arbidol showed selective antiviral activity against AdV-7, a DNA virus, only when added after infection (therapeutic index (TI) = 5.5) [1]. Arb interacts with the polar head-group of phospholipid at the membrane interface. Fluorescence studies of interactions between Arb and either tryptophan derivatives or membrane peptides reconstituted into liposomes show that Arb interacts with tryptophan in the micromolar range. Interestingly, apparent binding affinities between lipids and tryptophan residues are comparable with those of Arb IC50 of the hepatitis C virus (HCV) membrane fusion [2]. Arbidol not only prevented the cytopathic effect (CPE) of CVB(5), as demonstrated in an MTT colorimetric assay, when added during or after viral infection, with a 50% inhibitory concentration (IC(50)) from 2.66 to 6.62 microg/ml, but it also decreased the CVB(5)-RNA level in infected host cells, as shown in semi-quantitative RT-PCR [3].in vivo: Orally administered arbidol at 50 or 100 mg/kg/day beginning 24 h pre-virus exposure for 6 days significantly reduced mean pulmonary virus yields and the rate of mortality in mice infected with FLU-A (A/PR/8/34 H1N1) [1]. BALB/c mice were used as an animal model to test the Arbidol activity in vivo. Orally administered Arbidol at 50 mg/kg body weight/day (once a day) significantly reduced mean virus yields in the lungs and heart as well as mortality after infection for 6 days [3].
N-Acetylneuraminic acid-13C is the 13C labeled N-Acetylneuraminic acid.
EIDD-2801 is an orally bioavailable isopropylester prodrug of the ribonucleoside analog EIDD-1931. EIDD-2801 shows anti-influenza virus and coronaviruses activities. EIDD-2801 has the potential for seasonal and pandemic influenza treatment[1][2].
Antiviral agent 35 (compound 4d) is an orally active and potent influenza virus inhibitor, acting function in the early stage of virus replication. Antiviral agent 35 inhibits ROS accumulation, autophagy and apoptosis induced by influenza virus, and also inhibits inflammatory response mediated by RIG-1 pathway in mouse model with pulmonary infection. Antiviral agent 35 shows little cytotoxicity with CC50 >800 μM in MDCK cells, and anti-H1N1 (A/Weiss/43) activity with EC50 of 2.28 μM[1].
NDV-IN-1 is an antiviral agent with high neuraminidase inhibitory activity. NDV-IN-1 exhibits in vitro inhibitory activity against Newcastle disease virus (NDV). NDV-IN-1 significantly inhibits NDV infection of Vero cells by preventing the release of virus particles from infected cells[1].
1-Deoxymannojirimycin hydrochloride is a selective class I α1,2-mannosidase inhibitor with an IC50 of 20 μM. 1-Deoxymannojirimycin hydrochloride is also a N-linked glycosylation inhibitor and inhibits HIV‐1 strains. 1-Deoxymannojirimycin hydrochloride has antiviral activity[1][2].