antiviral agent 5

Antiviral agent 5 is a crucial intermediate utilized in the development of antiviral agents that specifically target 3C and 3CL proteases, which includes the SARS-CoV-2 M pro enzyme.

Antidepressant agent 5 is a 7-substituted tetrahydroisoquinoline derivative with antidepressant activity.Antidepressant agent 5 acts similarly to magnoflorine in the study of depression and can be used for the prevention and treatment of depressive disorders.

2H-Pyrido[2',1':3,4]pyrazino[1,2-b]indazole-3-carboxylic acid, 6-(1, 1-Dimethylethyl)-6, 7-Dihydro-10 -(3-methoxypropoxy)-2-oxo-, (6R)- has antibacterial and antiviral activity and can be used to study Hepatitis B virus.

Antiviral agent 17 is a nucleoside analog with antiviral and antiparasitic activity, inhibits hepatitis C virus 1B and inhibits Trypanosoma brucei and Trypanosoma brucei, and can be used in the study of viral infections and malignant diseases.

Antiviral agent is thiazolidin-4-one with anti-hepatitis B activity

Antiviral agent 34 is an orally available, potent antiviral compound that inhibits influenza A and B viruses.Antiviral agent 34 inhibits the proliferation of influenza viruses by modulating RNA polymerase.Antiviral agent 34 is used in the study of viral infections.

Antituberculosis agent-5 is a small molecule used for high-throughput assays.

Antiviral agent 27 (Compound 12) exhibits significant activity against the Ebola virus, with an EC50 value of 14 nM [1].

Anti-inflammatory agent 5 effectively inhibits nitric oxide (NO) production in lipopolysaccharide-induced BV-2 microglial cells.

Antiviral agent 33 (compound 1c), a double-stranded DNA (dsDNA) virus inhibitor, exhibits potent inhibitory activity with IC50 values of 0.0790 µM for VACV and 0.1572 µM for AdV5, and is a candidate for oral administration [1].

Anti-Influenza agent 5 (Compound IIB-2), a chalcone-like derivative, serves as an influenza nuclear export inhibitor. It effectively inhibits oseltamivir-resistant strains and hinders viral proliferation by obstructing the export of influenza virus nucleoprotein [1].

Antiviral agent 18 (Compound 5) shows good antiviral activity against murine norovirus. Antiviral agent 18 is an anti-infection agent that has the potential in infectious and malignant diseases research [1].

Antiviral agent 36 (compound 27), a potent inhibitor of both dengue (DENV) and Zika (ZIKV) viruses, demonstrates replication inhibition with EC50 values of 100 nM for ZIKV-FLR, 90 nM for ZIKV-HN16, 210 nM for DENV-2, and 120 nM for DENV-3 [1].

Antiviral agent 7 is a peptide-based coating that kills viruses.

Antiparasitic agent-5 (compound 8h) exhibits potent selectivity as an antiparasitic agent against Leishmania infantum (L. infantum), with an IC50 value of 2.50 μM. Additionally, this compound displays cytotoxic effects on HepG2 cells with a CC50 value of 6.78 μM [1].

GABAA Receptor Agent 5 (compound 018) serves as a potent γ-GABAAR antagonist, possessing a Ki of 0.020 μM. This compound exhibits γ-GABAAR antagonist properties, yet it demonstrates low cellular membrane permeability [1].

Antiviral agent 14 is an antiviral agent that inhibits tobacco mosaic virus (TMV) (EC50: 135.5 μg/mL), and cucumber mosaic virus (CMV) (EC50: 178.6 μg/mL).

Antiviral agent 20 (Compound 17b) is a selective inhibitor of Zika virus (EC50: 4.5 μM) and exhibits low cytotoxicity.

Antiviral Agent 23, an effective inhibitor of enterovirus 71 (EV71) with an EC50 value of 94 nM, also exhibits potent suppression of METTL3/METTL14 activity. This compound is employed in the research of infections.

Antiviral agent 25 (compound 6g), a novel non-peptide analog covalent inhibitor of SARS-CoV-2 3CL pro, exhibits robust inhibitory activity against both SARS-CoV-2 3CL pro and SARS-CoV-2 PL pro, with IC50 values of 0.118 µM and 0.448 µM, respectively. Furthermore, it demonstrates significant antiviral effects against SARS-CoV-2, achieving an EC50 value of 7.249 µM [1].

Antiviral agent 10 effectively inhibits the respiratory syncytial virus (RSV) [1], serving as a potent anti-viral compound.

Antiviral agent 19 (Compound 3) is a selective inhibitor of Zika virus (EC50: 1.3 μM) with low cytotoxicity.

Antiviral agent 8, surpassing lead compounds crocin-1 and crocin-2, has been identified as a potent and promising candidate with enhanced antiviral activities.

Antiviral agent 35 (compound 4d) serves as a potent orally active inhibitor of the influenza virus, targeting early stages of viral replication. It suppresses influenza-induced ROS accumulation, autophagy, and apoptosis, along with the inflammatory response mediated by the RIG-1 pathway in a mouse model of pulmonary infection. Its cytotoxicity is minimal in MDCK cells, displaying a CC50 greater than 800 μM, and possesses anti-H1N1 (A/Weiss/43) activity with an EC50 of 2.28 μM [1].

Antiviral agent 46, also known as compound 4, is a cannabidiol (CBD) derivative exhibiting anti-SARS-CoV-2 activity (IC50: 1.90 μM) and ACE2 inhibition (IC50: 1.37 μM) [1].

Anti-MRSA agent is a potent antagonist of MRSA (MIC50: 0.38 μg/mL) with low hERG activity (IC50: 40 μM). anti-MRSA agent also has low toxicity to mammalian cells and little potential to acquire bacterial resistance.

Antimicrobial Agent-5 is a potent antimicrobial agent that exhibits exceptional cell selectivity against both Gram-negative and Gram-positive bacteria. It inhibits the interaction between LPS (lipopolysaccharide) and the CD14/TLR4 (Toll-like receptor 4) receptor, demonstrating anti-inflammatory activity in combating LPS-induced inflammation.

Antiproliferative agent-5 (compound 4o) irreversibly and significantly inhibits the proliferation of gastric cancer cells. antiproliferative agent-5 blocks the cell cycle in G2/M phase, induces ROS accumulation and activates cellular autophagy. Antiproliferative agent-5 can be used in anti-cancer research.

Antioxidant agent-5 (compound D-6) is a potent antioxidant. antioxidant agent-5 inhibits oxLDL-induced increases in ROS levels and NF-κB nuclear translocation. antioxidant agent-5 inhibits oxLDL (oxidized LDL)-induced apoptosis (VECs). Antioxidant agent-5 activates the Nrf2/HO-1 antioxidant pathway and exhibits protective activity against oxLDL-induced endothelial damage.

Antiviral agent 43 (compound 16) serves as a potent, orally active inhibitor of influenza A virus entry, demonstrating efficacy by inhibiting the replication of the influenza A strains VH04-H5N1 and PR8-H1N1 with EC50 values of 240 nM and 72 nM, respectively [1].

Antiviral agent 9 exhibits potent efficacy against HIV-1 with an EC50 value of 0.006 nM, indicating extremely low concentrations are sufficient to inhibit the virus. Additionally, it demonstrates a selectivity index (SI) nearly 300 times higher than that of tenofovir alafenamide fumarate (TAF), outlining its superior selectivity and potential safety profile.

Antitrypanosal agent 5 is a selective anti-trypanosomal agent that acts on T. brucei (IC50: 1 nM) and HEK293 cells (IC50: 483.3 μM).

Antiviral agent 6 showed excellent anti-TSWV effects in vivo (EC50: 188 mg/L).

Antiviral Agent 30 (Example 118) is an active compound against HCV and RSV with an inhibitory concentration (IC 50) of greater than 25μM [1].

Nucleoside Derivatives - 6-Modified purine nucleosides; Drugs and Inhibitors

Antiviral agent 15 (Compound 15f) is a Clofazimine derivative with antiviral activity.Antiviral agent 15 inhibits rabies virus (EC50: 1.45 μM) and pseudotyped SARS-CoV-2 (EC50: 14.6 μM).

Antileishmanial agent-4 is a ribonucleoside analogue with potent activity against L.infantum and T.cruzi, having EC 50 values of 0.68 μM and 0.83 μM, respectively [1].

Anti-infective agent 5 (compound 74) is an orally active inhibitor of Trypanosoma cruzi exhibiting an IC50 value of 0.10 μM. In addition to its potent inhibitory effect, anti-infective agent 5 demonstrates efficacy in reducing parasite burden in vivo. Consequently, this compound holds promising potential for research pertaining to infection. [1]

1. Octyl Gallate is an antioxidant approved by the US Food and Drug Administration (FDA) as a food additive. 2. Octyl Gallate has antimetastatic activity. 3. Octyl Gallate shows antimicrobial activity against H. pylori, with a minimum inhibitory concentration (MIC) value of 125 ug/mL. 4. Combination therapy with octyl gallate and ferulic acid improves cognition and neurodegeneration in a transgenic mouse model of Alzheimer's disease.5. Octyl Gallate is a potential anticancer agent, it exhibited decreased MCF-7 & MDA-MB-231 survival and induced apoptosis, with IC50 value of 40 uM. 6. Octyl gallate (Octyl 3,4,5-trihydroxybenzoate) has antiviral activity, it shows an inhibitory effect on the growth of herpes simplex virus type 1 (HSV-1) in HEp-2 or Vero cells. 7. Octyl gallate shows antifungal activity against Saccharomyces cerevisiae ATCC7754 and Zygosaccharomyces bailii ATCC 60483.

BVDU 5′-Triphosphate is an antiviral agent labeled with 5′-Triphosphate that specifically targets viral DNA polymerase. It exhibits outstanding selectivity for varicella-zoster virus (VZV) and herpes simplex virus type 1 (HSV-1) owing to its phosphorylation by the virus-specific thymidine kinase.

2-deoxy-D-Glucose-13C6is intended for use as an internal standard for the quantification of 2-deoxy-D-glucose by GC- or LC-MS. 2-deoxy-D-Glucose is a glucose antimetabolite and an inhibitor of glycolysis.1,2It inhibits hexokinase, the enzyme that converts glucose to glucose-6-phosphate, as well as phosphoglucose isomerase, the enzyme that converts glucose-6-phosphate to fructose-6-phosphate.32-deoxy-D-Glucose (16 mM) induces apoptosis in SK-BR-3 cells, as well as inhibits the growth of 143B osteosarcoma cells cultured under hypoxic conditions when used at a concentration of 2 mg/ml.4,5In vivo, 2-deoxy-D-glucose (500 mg/kg) reduces tumor growth in 143B osteosarcoma and MV522 non-small cell lung cancer mouse xenograft models when used alone or in combination with doxorubicin or paclitaxel .6 1.Kang, H.T., and Hwang, E.S.2-Deoxyglucose: An anticancer and antiviral therapeutic, but not any more a low glucose mimeticLife Sci.78(12)1392-1399(2006) 2.Aft, R.L., Zhang, F.W., and Gius, D.Evaluation of 2-deoxy-D-glucose as a chemotherapeutic agent: Mechanism of cell deathBr. J. Cancer87(7)805-812(2002) 3.Ralser, M., Wamelink, M.M., Struys, E.A., et al.A catabolic block does not sufficiently explain how 2-deoxy-D-glucose inhibits cell growthProc. Natl. Acad. Sci. USA105(46)17807-17811(2008) 4.Liu, H., Savaraj, N., Priebe, W., et al.Hypoxia increases tumor cell sensitivity to glycolytic inhibitors: A strategy for solid tumor therapy (Model C)Biochem. Pharmacol.64(12)1745-1751(2002) 5.Zhang, X.D., Deslandes, E., Villedieu, M., et al.Effect of 2-deoxy-D-glucose on various malignant cell lines in vitroAnticancer Res.26(5A)3561-3566(2006) 6.Maschek, G., Savaraj, N., Priebe, W., et al.2-deoxy-D-glucose increases the efficacy of adriamycin and paclitaxel in human osteosarcoma and non-small cell lung cancers in vivoCancer Res.64(1)31-34(2004)

(E)-5-(2-Bromovinyl)uracil (BVU) is a pyrimidine base and an inactive metabolite of the antiviral agents sorivudine and (E)-5-(2-bromovinyl)-2'-deoxyuridine (BVDU) that may be regenerated to BVDU in vivo. BVU irreversibly inactivates dihydropyrimidine dehydrogenase (DPD) in an NADPH-dependent manner. It enhances the efficacy of the chemotherapeutic agent and DPD substrate 5-fluorouracil in a P388 murine leukemia model when administered at a dose of 200 μmol/kg, increasing survival time.

XSJ2-46, a 5'-amino NI analog, is an antiviral agent possessing anti-Zika virus properties and demonstrates reasonable inhibition of RNA-dependent RNA polymerases (RdRp), with an IC50 of 8.78 μM [1].

Retro-2 cycl is a dihydroquinazolinone (DHQZ) retrograde trafficking inhibitor. Retro-2 cycl (RN 1-001) inhibits JCPyV and HPV16 pseudovirus(IC50s of 54 μM and 160 μM, respectively),with antiviral agent.

(-)-5′-Noraristeromycin is an antiviral agent. (-)-5′-Noraristeromycin also is an enantiomer of 5'-noraristeromycin and can inhibit intracellular HBV replication and virion production. (-)-5′-Noraristeromycin can be used in cancer research[1].

TMV-IN-5 (compound 1a) serves as an antiviral/antifungal agent, specifically targeting and inhibiting the assembly of the tobacco mosaic virus (TMV) by binding to its coat protein (CP), hence its potential application in pesticide formulation [1].

Nucleoside Derivatives - 5-Modified pyrimidine nucleosides; Azido-nucleosides; 2’,3’-Dideoxy nucleosides; Drugs and Inhibitors; Antiviral agent

L-I-OddU, a potent and selective anti-Epstein-Barr virus (EBV) agent, is a L-5'-halo-dioxolane nucleoside analogue. It demonstrates antiviral activity by effectively suppressing replicative EBV DNA and viral protein synthesis [1] [2]. With an EC 50 value of 0.03 μM, L-I-OddU exhibits high potency against EBV while maintaining low cytotoxicity, as indicated by its CC 50 value of 1000 nM.