antiviral agents

Idoxuridine (Dendrid) is an analog of DEOXYURIDINE that inhibits viral DNA synthesis. The drug is used as an antiviral agent.

Tenofovir (GS 1278) is an adenine analog REVERSE TRANSC-RIPTASE INHIBITOR with antiviral activity against HIV-1 and HEPATITIS B. It is used to treat HIV INFECTIONS and CHRONIC HEPATITIS B, in combination with other ANTIVIRAL AGENTS, due to the emergence of ANTIVIRAL DRUG RESISTANCE when it is used alone.

Daclatasvir dihydrochloride (BMS-790052 dihydrochloride) is an orally available antiviral agent that inhibits the NS5A region of the hepatitis C virus (HCV) and is used in combination with other oral antivirals to treat chronic hepatitis C. Elevations in serum enzyme levels during daclatasvir therapy are uncommon, and it has not been convincingly implicated in cases of clinically apparent liver injury with jaundice.

Darunavir (TMC114) is an HIV PROTEASE INHIBITOR that is used in the treatment of AIDS and HIV INFECTIONS. Due to the emergence of ANTIVIRAL DRUG RESISTANCE when used alone, it is administered in combination with other ANTI-HIV AGENTS.

2'-Deoxy-2'-fluorouridine serves as an intermediate in the synthesis of antiviral agents targeting influenza viruses[1].

2,5-Pyridinedicarboxylic Acid is used in the preparation of new derivatives as antiviral agents.

4-(3-chlorophenyl)-2,3-dihydro-1,3-thiazol-2-one has been used as a starting material for the synthesis of a variety of biologically active compounds, including antifungal, antiviral and anti-inflammatory agents.

6-ethenylquinoline is a structurally unique aromatic heterocyclic compound that is an important intermediate in the production of other aromatic compounds. It has also been used as a starting material for the synthesis of a variety of drugs, including antifungal, antiparasitic and antiviral agents. It has been shown to be an inhibitor of a variety of enzymes involved in drug metabolism, including cytochrome P450, aldehyde oxidase and xanthine oxidase.

5-Et-ddU, Structure-activity relationships of pyrimidine nucleosides as antiviral agents for human immunodeficiency virus type 1 in peripheral blood mononuclear cells.

Darunavir Ethanolate (UIC 94017) is an HIV PROTEASE INHIBITOR that is used in the treatment of AIDS and HIV INFECTIONS. Due to the emergence of ANTIVIRAL DRUG RESISTANCE when used alone, it is administered in combination with other ANTI-HIV AGENTS.

(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), which can be regenerated to BVDU in vivo. BVU irreversibly inactivates dihydropyrimidine dehydrogenase (DPD) in an NADPH-dependent manner, enhancing 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, thereby increasing survival time.

Methyl 3,4-dihydroxyphenylacetate is a polyphenol found in I. aquifolium seeds, exhibiting antioxidant and antiviral activities. It scavenges 2,2-diphenyl-1-picrylhydrazyl radicals in a cell-free assay (IC50 = 0.0025 mg ml) and inhibits enterovirus 71 replication in rhabdomyosarcoma cells (0.01 μg ml).

4-(N-Boc-amino)piperidine is an organic building block.1,2It has been used in the synthesis of aminopiperidine antiviral chemokine (C-C motif) receptor 5 (CCR5) antagonists and antibacterial agents. 1.Burrows, J.N., Cumming, J.G., Fillery, S.M., et al.Modulators of the human CCR5 receptor. Part 1: Discovery and initial SAR of 1-(3,3-diphenylpropyl)-piperidinyl amides and ureasBioorg. Med. Chem. Lett.15(1)25-28(2005) 2.Reck, F., Alm, R., Brassil, P., et al.Novel N-linked aminopiperidine inhibitors of bacterial topoisomerase type II: Broad-spectrum antibacterial agents with reduced hERG activityJ. Med. Chem.54(22)7834-7847(2011)

Ribavirin-13C5is intended for use as an internal standard for the quantification of ribavirin by GC- or LC-MS. Ribavirin is an antiviral guanosine nucleoside analog.1,2Upon entry into cells, ribavirin is metabolized to an active triphosphate form that induces viral RNA chain termination and inhibits viral polymerases. It reduces replication in a panel of seven RNA and four DNA viruses in Vero cells (EC50s = 2-95 μg/ml).3Ribavirin also reduces replication of severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2) in Vero cells (EC50= 109.5 μM).4Aerosol administration of ribavirin (30 mg/kg) reduces mortality in a mouse model of influenza A infection.5Formulations containing ribavirin have been used in the treatment of respiratory syncytial virus (RSV), hepatitis C virus (HCV), and viral hemorrhagic fevers. 1.Gilbert, B.E., and Knight, V.Biochemistry and clinical applications of ribavirinAntimicrob. Agents Chemother.30(2)201-205(1986) 2.Gordon, C.J., Tchesnokov, E.P., Woolner, E., et al.Remdesivir is a direct-acting antiviral that inhibits RNA-dependent RNA polymerase from severe acute respiratory syndrome coronavirus 2 with high potencyJ. Biol. Chem.295(20)6785-6797(2020) 3.Kirsi, J.J., North, J.A., McKernan, P.A., et al.Broad-spectrum antiviral activity of 2-β-D-ribofuranosylselenazole-4-carboxamide, a new antiviral agentAntimicrob. Agents Chemother.24(3)353-361(1983) 4.Wang, M., Cao, R., Zhang, L., et al.Remdesivir and chloroquine effectively inhibit the recently emerged novel coronavirus (2019-nCoV) in vitroCell Res.30(3)269-271(2020) 5.Wilson, S.Z., Knight, V., Wyde, P.R., et al.Amantadine and ribavirin aerosol treatment of influenza A and B infection in miceAntimicrob. Agents Chemother.17(4)642-648(1980)

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.

Ensitrelvir (S-217622) fumarate is a novel orally active inhibitor targeting the SARS-CoV-2 3CL protease (IC50 = 13 nM), demonstrating non-covalent and non-peptidic characteristics. This compound represents a pioneering advancement in the development of effective antiviral agents against the SARS-CoV-2 virus.

Deleobuvir sodium is the salt form of Deleobuvir, also known as BI207127, a non-nucleoside hepatitis C virus NS5B polymerase inhibitor for the treatment of hepatitis C. Deleobuvir was tested in combination regimens with pegylated interferon and ribavirin, and in interferon-free regimens with other direct-acting antiviral agents including faldaprevir. Deleobuvir showed that a triple combination of deleobuvir, faldaprevir, and ribavirin performed well in HCV genotype 1b patients. Efficacy fell below 50%, however, for dual regimens without ribavirin and for genotype 1a patients. In December 2013, deleobuvir was discontinued since recent findings from phase III trials did not suggest sufficient efficacy.

Thiocarbazate, also known as CID16725315, is an inhibitor of human cathepsin L. Inhibition of cathepsin L thus holds promise for therapeutic intervention for both SARS-CoV and Ebola virus infection. With respect to the development of antiviral agents, inhibitors of human cathepsin L are not subject to resistance because of rapid mutations of the viral genome. Cathepsin L is therefore an attractive target for drug development.

3'-DMTr-dG(iBu) is a nucleoside used in the synthesis of nucleic acids, including antiviral agents for researching viral infections (HBV, HDV) and oligonucleotides aimed at combating Alzheimer's disease and other tauopathies [1].