Antiviraux

<p>Emtricitabine is an antiviral drug that is used to treat chronic viral hepatitis, which is caused by the hepatitis B and C viruses. The drug blocks the activity of reverse transcriptase, which is an enzyme necessary for the replication of viral RNA in the body. Emtricitabine has been shown to be effective against acute hepatitis B virus infection and chronic hepatitis B virus infection with or without cirrhosis. It also has been shown to be effective against chronic hepatitis C virus infection with or without cirrhosis.</p>

Tenofovir diphosphate triethylamine (mixture of diastereomers) is an antiviral compound, which is a synthetic chemical product derived from the parent compound, tenofovir. This formulation includes a mixture of diastereomers to enhance its solubility and bioavailability. The compound primarily functions as a nucleotide reverse transcriptase inhibitor (NRTI). It targets viral reverse transcriptase enzymes, inhibiting DNA synthesis and subsequent viral replication by causing premature chain termination.

<p>Cytarabine is also known as cytosine arabinoside (ara-C) and is a chemotherapy drug that works by inhibiting DNA synthesis. It acts as a nucleoside analogue, which is incorporated into the growing DNA chain during replication. Cytarabine combines a cytosine base with an arabinose sugar (1β-arabinofuranosylcytosine) and is an analog for human deoxycytosine. Cytarabine interferes with DNA synthesis as it is rapidly converted to cytosine arabinoside triphosphate, damaging DNA when cells are in the synthesis phase (S phase). Tumor cells which are highly mitotic and growing rapidly are therefore preferably targeted. Cytarabine also inhibits nucleotide reductase enzymes as well as nuclear polymerases, leading to interruption and inhibition of synthesis, strand breaks and cell death.</p>

<p>Emtricitabine is a nucleoside analog that is an antiviral drug used to treat HIV/AIDS. It is a synthetic nucleoside analog of cytidine, in which the 3' phosphate and 5' hydroxyl groups have been replaced with a fluorine atom and a methoxy group, respectively. Emtricitabine has been shown to inhibit the synthesis of viral DNA by competing for incorporation into the viral DNA strand during the elongation phase of viral replication. Emtricitabine also has anticancer activity, but no other known therapeutic uses.</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>Etravirine is a non-nucleoside reverse transcriptase inhibitor (NNRTI) medication used in the treatment of human immunodeficiency virus (HIV) infections. It works by blocking reverse transcriptase, an enzyme essential for replication of the virus, thereby preventing the virus from multiplying and spreading. Etravirine is often used in combination with other antiretroviral drugs to effectively treat HIV/AIDS. It is commonly prescribed for patients with virus strains that are resistant to other NNRTI medications due to mutations that confer resistance- mutations K103N and Y181C. Etravirine is a diarylpyrimidine (DAPY) and has conformational isomerism meaning that it binds reverse transcriptase in an fleible manner, under multiple conformations. The impact of specific point mutations in the virus is therefore lessened.</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>

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>Applications (R)-(((1-(6-Amino-9H-purin-9-yl)propan-2-yl)oxy)methyl)phosphonic Acid Methyl Ester Trimethylamine is an intermediate in the synthesis of Tenofovir (T018500), is an acyclic phosphonate nucleotide analogue.<br>References Peng, J., et al.: J. Clin. Pharmacol., 46, 265 (2006), Seminari, E., et al.: J. Antimicrob. Chemother., 60, 831 (2007),<br></p>

<p>Applications (S)-(5S,6S,8S)-5,8-Dibenzyl-12,12-dimethyl-3,10-dioxo-1-(thiazol-5-yl)-2,11-dioxa-4,9-diazatridecan-6-yl 2-(3-((2-Isopropylthiazol-4-yl)methyl)-3-methylureido)-3-methylbutanoate is an protected prodrug of Ritonavir (R535000), which is a selective HIV protease inhibitor.<br></p>

<p>Applications (S)-Isopropyl 2-(((R)-(((2R,3R,4R,5R)-3-((tert-Butyldimethylsilyl)oxy)-5-(2,4-dioxo-3,4-dihydropyrimidin-1(2H)-yl)-4-fluoro-4-methyltetrahydrofuran-2-yl)methoxy)(phenoxy)phosphoryl)amino)propanoate is an intermediate in the synthesis of Sofosbuvir (R)-Phosphate (S675615), which is an impurity of PSI-7977 (P839640), a prodrug that is metabolized to the active antiviral agent 2'-deoxy-2'-α-fluoro-β-C-methyluridine-5'-monophosphate and is currently being investigated in phase 3 clinical trials for the treatment of hepatitis C. Studies have profiled PSI-7977 as a nucleotide inhibitor of hepatitis C virus, exerting selective inhibitory effects towards HCV NS5B polymerase.<br>References Lam, A.M.,et al.: Antimicrob. Agents. Chemotherapy., 56, 3359 (2012); Lam, A.M., et al.: J. Virol., 85, 12334 (2011); Sofia, M.J., et al.: J. Medn. Chem., 53, 7202 (2010)<br></p>

<p>Applications 2-Hydroxy-2-methylpropanethioamide is an thioamide compound integrated as an constituent in the synthesis of Ritonavir (R535000) and its derivatives.<br></p>

<p>Applications A highly reactive thiol-specific spin-label. A specific conformational probe of thiol site structure by virtue of its minimal rotational freedom and distance from the covalent disulfide linkage to the macromolecule under study.<br></p>

<p>Applications Used in the synthesis of enantioselective synthesis of carbocyclic ribavirin, its analogs and other antiviral agents.<br>References Kuang, R. et al.; Tetrahedron Lett. 41, 9575 (2000)<br></p>

<p>Applications Intermediate in the preparation of α-Ribavirin.<br></p>

<p>Applications Intermediate in the preparation of Ribavirin.<br></p>

<p>Applications (S)-2-(3-((2-(2-Hydroxypropan-2-yl)thiazol-4-yl)methyl)-3-methylureido)-3-methylbutanoic Acid Methyl Ester is an intermediate in the synthesis of Ritonavir (R535000) derivatives.<br></p>

<p>Applications (S)-2-(3-((2-(2-Hydroxypropan-2-yl)thiazol-4-yl)methyl)-3-methylureido)-3-methylbutanoic Acid is an intermediate in the synthesis of Ritonavir (R535000) derivatives.<br></p>