Antivirals

<p>Rilpivirine (R278474) is a diarylpyrimidine derivative and reverse transcriptase inhibitor with antiviral activity against HIV-1 that is used in the treatment</p>

<p>HIV-1 Nef-IN-1 is an inhibitor of HIV-1 Nef protein. It efficiently competes for Nef-SH3Hck interactions(Kd : 6.7 μM).</p>

<p>Azvudine hydrochloride (RO-0622 hydrochloride) is an NRTI inhibitor with antiviral activity, inhibiting HIV, HBV and HCV.</p>

<p>Amantadine (1-Aminoadamantane), an antiviral, is a weak antagonist of the NMDA-type glutamate receptor, increases dopamine release and blocks dopamine reuptake.</p>

<p>Bemnifosbuvir (AT-511) is a novel phosphoramidate prodrug of 2'-fluoro-2'-C-methylguanosine-5'-monophosphate that has potent in vitro activity against HCV.</p>

<p>1-Deoxynojirimycin hydrochloride (Moranoline) is a potent and selective inhibitor of alpha-glucosidase, most commonly found in mulberry leaves.</p>

<p>BMS-707035 is a specific HIV-I integrase (IN) inhibitor with IC50 of 15 nM. Phase 2.</p>

<p>ML-SA1 (Mucolipin synthetic agonist 1) is a selective TRPML agonist, inhibits DENV2 and ZIKV by promoting lysosomal acidification and protease activity.</p>

<p>3-Methoxyflavone is a Flavonoids, with antiviral activity</p>

<p>Rose Bengal sodium is a potent inhibitor of VGlut and vesicular monoamine transporter (VMAT) (Ki of 19 and 64 nM for VGlut andVMAT, respectively）</p>

<p>Adefovir: acyclic nucleoside phosphonate, reverse transcriptase inhibitor for hepatitis B and herpes treatment.</p>

<p>Aplidine possesses antiviral activity against SARS-CoV-2(IC90 = 0.88 nM).</p>

<p>Dryocrassin ABBA (Dryocrassin) is a flavonoid natural product derived from Dryopteris crassirhizoma, with antiviral and antibacterial activities.</p>

<p>AKOS B018304 is an arylalkylidene derivative with polar substitution at para-position.</p>

<p>Bonafton (Bonaphthone) is an antiviral agent.</p>

<p>1-Deoxynojirimycin (Moranoline) is a potent α-glucosidase inhibitor, suppressing postprandial blood glucose, thereby possibly preventing diabetes mellitus.</p>

<p>Isoborneol (DL-Isoborneol) is a monoterpene alcohol, with neuroprotective and antiviral activities</p>

<p>Robinetin (3,3',4',5',7-Pentahydroxyflavone) has antioxidant and antiradical activities, inhibits EYPC membrane lipid peroxidation and HbA glycosylation with</p>

<p>Bemnifosbuvir hemisulfate (AT-527) is a potent inhibitor of HCV virus replication.</p>

<p>2,2'-Anhydrouridine (2,2'-Cyclouridine) is a research tool for antiviral and anticancer studies.</p>

<p>FIT-039 is a selective and ATP-competitive, orally active inhibitor of CDK9( IC50 : 5.8 μM;CDK9/cyclin T1).</p>

<p>6-azathymine inhibits D-3-aminoisobutyrate-pyruvate aminotransferase; 6-azauracil competes with beta-alanine, uncompetitive with pyruvic acid, Ki ~8.9 mM.</p>

<p>(-)-Arctigenin ((-)-Arctigenin) is found in burdock.</p>

<p>AG-1478 (NSC-693255) (Tyrphostin AG-1478) is a selective EGFR inhibitor.</p>

<p>BVDV-IN-1 is a non-nucleoside inhibitor (NNI) of bovine viral diarrhea virus (BVDV), with an EC50 of 1.8 μM.</p>

<p>DL-Serine is a non-essential amino acid and a natural ligand and allosteric activator of pyruvate kinase M2.</p>

<p>L-Chicoric Acid (trans-Caffeoyltartaric acid) has been shown to inhibit hyaluronidase and HIV-1 integrase, and to possess phagoeytosis stimulatory activity.</p>

<p>Cidofovir ((S)-HPMPC) 通过特异性抑制病毒 DNA 合成来抑制病毒复制。</p>

<p>Dodecyl gallate (Progallin LA) is the ester of gallic acid and dodecanol. As a food additive, it is used as a preservative and antioxidant.</p>

<p>Chelidonine from Chelidonium majus triggers HeLa cell apoptosis, may reverse MDR, boost chemotherapeutics against leukemia, and inhibit cancer cell metastasis.</p>

<p>Gossypin exhibits multiple medicinal properties and inhibits NF-kappaB, reducing inflammation, cancer growth, and angiogenesis.</p>

<p>Brincidofovir (HDP-CDV) is an orally active, lipophilic form of cidofovir.</p>

<p>Diphyllin could be characterized as a new V-ATPase inhibitor in treating gastric cancer and inhibiting the phosphorylation of LRP6 in Wnt/β-catenin signaling.</p>

<p>Applications Antiviral nucleoside analog, also an impurity found in emtricitabine (E525000).<br>References Jeong, L., et al.: J. Med. Chem., 36, 181 (1993),<br></p>

<p>Impurity Atazanavir Impurity (Pyridinyl Benzoic Acid)<br>Applications Reactive metabolite of Atazanavir (A790051). Atazanavir Impurity (Pyridinyl Benzoic Acid)<br>References Li, F. et al. Drug Metab. Disp., 39, 294 (2011);<br></p>

<p>Braco-19 is a telomerase/telomere inhibitor and an inhibitor of HAdV viral replication with antiviral activity that reduces lipid vacuolization in adipocytes, inhibits proliferation and decreases telomerase activity in human glioblastoma cells.</p>

<p>2'-C-beta-Methylguanosine (2'-C-Methylguanosine), with antiviral activity, inhibits dengue virus 2.</p>

<p>Impurity Atazanavir Impurity C<br>Applications Atazanavir intermediate. Enantiomer R. Atazanavir Impurity C<br>References Vassar, R., et al.: Science, 286, 735 (1999), Maillard, M., et al.: J. Med. Chem., 50, 776 (2007), Stauffer, S., et al.: Bioorg. Med. Chem. Lett., 17, 1788 (2007),<br></p>

<p>Impurity Adapalene USP Related Compound B<br>Applications Adapalene intermediate, an ester of Adapalene. Adapalene USP Related Compound B.<br>References Charpentier, B., et al.: J. Med. Chem., 38, 4993 (1995),<br></p>

<p>Applications Indinavir Sulfate is a member of the novel hydroxyaminopentane amide class of HIV-1 protease inhibitors. Antiviral. It is a COVID19-related research product.<br>References Vacca, J.P., et al.: Proc. Nat. Acad. Sci. USA, 91, 4096 (1994), Dorsey, B. D., et al.: J. Med. Chem., 37, 3443 (195), Balani, S.K., et al.: Drug Metab. Dispos., 23, 266 (1995)<br></p>

<p>Impurity Oseltamivir EP Impurity D<br>Applications 4-Acetylamino-3-hydroxybenzoic Acid Ethyl Ester (Oseltamivir EP Impurity D) is an impurity in the antiviral drug Oseltamivir (O700100).<br></p>

<p>Applications Elenolic Acid is an antiviral agent that inhibits reverse transcriptases, inhibited the growth of chicken embryo fibroblast cells as well as Escherichia coli and Bacillus subtilis strains.<br>References Heinze, J.E., et al.: Antimicrob. Agents Chemother., 8, 421 (1975); Renis, H,E..: Antimicrob. Agents Chemother., 8, 149 (1975)<br></p>

<p>Peramivir is a neuraminidase inhibitor used to treat influenza by preventing virus release from cells.</p>

<p>Ganciclovir is an acyclovir analog that is used in the treatment of cytomegalovirus and herpetic keratitis of the eye. This drug is a DNA polymerase inhibitor and exhibits its anti-viral properties by inhibiting viral replication.</p>

<p>Adefovir is an antiviral drug that is used for the treatment of hepatitis B infections. This drug works by blocking the enzyme reverse transcriptase, therefore preventing the replication of the virus in the body.</p>

<p>Abacavir is an antiviral nucleoside reverse transcriptase inhibitor that is used for the treatment of HIV. This drug inhibits the activity of HIV-1 reverse transcriptase (RT) both by competing with dGTP and by its incorporation into viral DNA.</p>

<p>Viramidine is a nucleotide analogue prodrug, which is derived from naturally occurring nucleosides, specifically optimized for enhanced therapeutic profiles. Its mode of action involves conversion into ribavirin triphosphate within the body. This active form inhibits viral RNA polymerase, a critical enzyme necessary for viral replication. By disrupting the synthesis of viral RNA, Viramidine effectively reduces viral proliferation within host cells.</p>

<p>Cidofovir is an anti-viral agent that is used to treat Cytomegalovirus (CMV) retinitis in patients with AIDS. This drug suppresses CMV replication by inhibiting viral DNA synthesis.</p>

<p>Non-nucleoside reverse transcriptase inhibitor; antiviral agent against HIV</p>

<p>Stavudine is an antiviral, reverse transcriptase inhibitor that is used to treat HIV/AIDS. It belongs to the group of nucleoside analogues of thymidine that is converted into stavudine monophosphate. Stavudine works by inhibiting viral replication by preventing the incorporation of viral dNTPs into the growing DNA chain, thus blocking DNA synthesis.</p>

<p>Ritonavir is a HIV protease inhibitor. It has an anti-retroviral activity as it inhibits the protease enzymes specific of both HIV-1 and HIV-2 and has been shown to be effective in controlling virus replication in humans and animals. Ritonavir works by preventing the HIV viral protease enzyme from cleaving the structural and replicative proteins produced by HIV genes such as gag and pol.</p>

<p>Anti-viral; thymidine analogue; DNA plymerase inhibitor</p>

<p>Inhibitor of HIV-1 integrase strand transfer; antiviral</p>

<p>Anti-viral; HIV protease inhibitor</p>

<p>Nucleoside analog with antiviral activity against zoonotic feline infectious peritonitis virus (FIPV) and severe acute respiratory syndrome (SARS) virus from Coronaviridae family. The compound is a pro-drug and undergoes intracellular phosphorylation resulting in the active triphosphate metabolite. The triphosphorylated GS 441524 analog competes with natural nucleoside triphosphates and interferes with viral RNA synthesis. In previous studies it was tested in vitro as well as in experimental animals and showed good safety profile.</p>

<p>Darunavir is an HIV protease inhibitor that is used in the treatment of HIV-1 infection. This drug inhibits HIV-1 protease from binding and catalyzing by attaching to the enzyme and preventing HIV replication.</p>

<p>Efavirenz is a non-nucleoside-based reverse transcriptase inhibitor (NNRTI) of the reverse transcriptase of HIV-1. It inhibits the viral enzyme reverse transcriptase by binding to its active site. In certain cell culture assays, Efavirenz showed great efficiency when inhibiting wild-type HIV-1 replication. In the treatment of HIV, Efavirenz has been studied in combination with Emtricitabine and Tenofovir disoproxil fumarate for ease of administration in some clinical studies. Recent in vitro cell studies indicated Efavirenz is a potential treatment for pancreatic, prostate and triple-negative breast cancers due to its cytotoxicity against cancer cells.Efavirenz is part of our Bio-X ™ Range. These products are aimed at life science researchers who need high quality ready to use products for assay development, screening or other R&amp;D work. With a solubility datasheet and convenient vials, all of our Bio-X ™ products are in stock across our global warehouses for rapid delivery and ease of use.</p>

<p>**Ivermectin 8α-hydroperoxide** is a derivative of the antiparasitic agent ivermectin, which is synthesized through chemical modification. Ivermectin originally derives from the fermentation products of the bacterium *Streptomyces avermitilis*. The modification to form 8α-hydroperoxide involves the addition of a hydroperoxide group, potentially altering its biological properties.</p>

<p>EIDD 2801 is an orally bioavailable prodrug of β-D-N4-hydroxycytidine and was shown to inhibit SARS-CoV-2 replication in human airway epithelial cells. EIDD 2801 was also tested in mice infected with SARS-CoV and MERS-CoV viruses. EIDD 2801 targets the RNA-dependent RNA polymerase (RdRp) and reduces virus titer and improved pulmonary function in experimental animals when used in prophylactic and therapeutic regime.</p>

<p>Filociclovir is a novel antiviral agent, which is synthesized from small-molecule pharmaceutical compounds. It functions primarily by inhibiting viral DNA polymerase, thereby halting viral replication within infected host cells. This mechanism of action is particularly effective against certain herpesviruses, as it targets the polymerase enzyme that is critical for viral DNA synthesis and proliferation.</p>

<p>Pimodivir is a non-nucleoside-derived inhibitor of the polymerase basic protein 2 (PB2) subunit found in the polymerase complex of the influenza A virus. In general, pimodivir is indicated for the treatment of patients with severe influenza although knowledge about possible rise of resistance is not available.</p>

<p>Inhibitor of viral protein NS5B</p>

<p>BMS 806 is an antiretroviral agent and is used for the treatment of HIV. It inhibits the fusion of the HIV virus with the host cell membrane.</p>

<p>Inhibitor of hepatitis C viral enzyme NS3-4A serine protease</p>

<p>Raltegravir is an antiretroviral agent that is used for the treatment of HIV infections. It inhibits HIV integrase in order to prevent viral genome from being inserted into the human genome. It binds to the active site of the enzyme and prevents it from binding to a target sequence on the viral DNA. This drug is metabolized by glucuronidation.</p>

<p>Selective and potent inhibitor of sialidases (neuraminidases) in influenza A and B viruses. The compound binds tightly to the viral neuraminidase active site in late stages of viral life-cycle. It inhibits shedding sialic acids from host cell surface glycans, which interact with viral hemagglutinin, and consequently prevents release of new viral particles from the host cell surface.</p>

<p>PI4KIII beta inhibitor</p>

<p>Lamivudine (commonly called 3TC) is a potent nucleoside analogue reverse transcriptase inhibitor. It is one of the front line treatments for HIV.  It is an analogue of cytidine, and can inhibit both types (1 and 2) of HIV reverse transcriptase as well as the reverse transcriptase of hepatitis B. It needs to be phosphorylated to its triphosphate form before it is active.</p>

<p>Saquinavir is a HIV protease inhibitor drug that is used with other antiretroviral drugs for the treatment of HIV-1. As this drug prevents HIV protease activity, it prevents the proteolysis of the Gag polyprotein and thus results in non-infectious virus particles.</p>

<p>Anti-viral; non-nucleoside reverse transcriptase inhibitor</p>

<p>Baloxavir marboxil is a selective inhibitor of the cap-dependent endonuclease of RNA polymerase, an acidic protein in influenza A and B viruses. In patients, baloxavir marboxil reduces the time to recovery by alleviating the symptoms of the influenza A and B infection, in both adults and children.</p>

<p>Raltegravir is an antiretroviral agent used for the treatment of HIV infections in conjunction with other antiretrovirals. It inhibits the activity of HIV-1 integrase, which impedes the insertion of HIV-1 DNA into the host cell genome. Raltegravir also inhibits resistant mutants of HIV-1 that are associated with disease activity and progression.</p>

<p>Triazavirin is an antiviral drug developed against SAR-CoV-2. The action of triazavirin might be due to its ability to inhibit the Mpro protease from SARS viruses. Triazavirin has been clinically tested in the treatment of COVID-19 patients.</p>

<p>Anti-viral; NS5A protein inhibitor</p>

<p>Anti-viral; NS3/4A protease inhibitor_x000D_</p>

<p>Chemically derived from ritonavir, Lopinavir belongs to the amphetamines. Lopinavir is clinically used in the prevention and treatment of HIV infections as it acts as HIV-1 protease inhibitor. In 2020, lopinavir was tested to treat COVID-19 patients and although it led to a higher rate of gastrointestinal side effects, the Lopinavir-treated group had a lower incidence of severe complications. Overall it was deemed not to work as a treatment.</p>

<p>Darunavir is a HIV-1 protease inhibitor used orally in the treatment of patients with multi-drug resistant HIV-1 infection (Ghosh, 2007). It has also been shown to be effective against other infectious diseases such as hepatitis C virus and SARS coronavirus. Metabolized by cytochrome P450 3A (CYP3A) isoenzymes, darunavir is often administered together with ritonavir that prolongs its bioavaiability, giving a terminal elimination half-life (t1/2) of 15 hours (Back, 2008). The effect of darunavir on natural compounds such as matrix proteins and toll-like receptor activity has also been studied via high performance liquid chromatography (HPLC) experiments.</p>

<p>Cytarabine is a pyrimidine nucleoside analogue that is used to treat leukaemia especially, non-lymphocytic leukaemia. This drug also has anti-viral and immunosuppressant properties. Cytarabine is cytotoxic and acts through direct DNA damage. Although its mechanism of action is not fully understood, it is said to inhibit DNA polymerase.</p>

<p>Nucleoside analog with antiviral activity against coronaviruses, hepatitis and influenzas viruses. EIDD 1931 inhibited the Middle East Respiratory Syndrome coronavirus (MERS-CoV) and the murine hepatitis virus (MHV) replication in vitro at submicromolar concentrations. EIDD 1931 is able to evade the proofreading exonuclease ExoN and presents with high barrier to development of drug resistance.</p>

<p>Anti-viral; non-nucleoside reverse transcriptase inhibitor</p>

<p>Rupintrivir is a peptidomimetic antiviral with action on rhinovirus 3C protease to inhibit viral replication and is used for research on rhinovirus and other viral infections.</p>

<p>Nucleoside reverse transcriptase inhibitor; anti-Hepatitis B virus</p>

<p>Anti-viral; RNA polymerase inhibitor; sofosbuvir metabolite</p>

<p>Potent inhibitor of viral RNA polymerase called non-structural protein 5B (NS5B). This nucleotide analog is effective against Hepatitis C virus (HCV) infection since it inhibits viral RNA replication. Sofosbuvir is a prodrug and gets triphosphorylated in the liver cells, generating biologically active compound with anti-viral activity.</p>

<p>Zalcitabine (also known as dideoxycytidine or ddC) is a nucleoside analogue reverse transcriptase inhibitor (NRTI) medication used in the treatment of human immunodeficiency virus (HIV) infections. It works by blocking reverse transcriptase, an enzyme essential for replication of the HIV virus, thereby preventing the virus from multiplying and spreading. Zalcitabine is often used in combination with other antiretroviral drugs to effectively treat HIV/AIDS.</p>

<p>Anti-viral; HIV protease inhibitor</p>

<p>Ombitasvir is a NS5A inhibitor antiviral agent with action on hepatitis C virus replication and is used for treating chronic hepatitis C in combination therapies.</p>