Track topics on Twitter Track topics that are important to you
GSK3082 - a hepatitis C virus RNA polymerase inhibitor - and a series of analogues with structural diversity at the 5-position were prepared from a 2,2,4,5-tetrasubstituted pyrrolidine obtained with a well-defined stereochemistry from the 1,3-dipolar cycloaddition of the chiral imino ester derived from leucine tert-butyl ester and (R)-2,3-O-isopropylideneglyceraldehyde with methyl acrylate. The chiral 2,2-dimethyl-1,3-dioxolane moiety provided by the glyceraldehyde served as a synthetic equivalent for different substituents and functional groups and these transformations usually required mild reaction conditions and simple work-up procedures. The inhibitory activity of the resulting GSK3082 analogues was studied in vitro in a cell-based assay of the subgenomic HCV RNA replication system. Some of the analogues showed good inhibitory activity with IC50 values in the nanomolar concentration range.
This article was published in the following journal.
Name: European journal of medicinal chemistry
Hepatitis C virus (HCV) affects approx. 3% of the world's population and accounts for ca 300 000 deaths per year. 80% of individuals with HCV develop chronic symptoms which, when untreated, may caus...
ABBV-168 is a dihalogenated nucleotide under investigation for the treatment of hepatitis C virus (HCV). Three synthetic routes aimed at achieving the stereoselective installation of the C2' gem-Br,F ...
In continuation of our efforts toward the discovery of potent non-nucleoside HBV inhibitors with novel structures, we have explored the solvent-exposed protein region of heteroaryldihydropyrimidines (...
Synthesis and Anti-HCV Activities of 4'-Fluoro-2'-Substituted Uridine Triphosphates and Nucleotide Prodrugs: Discovery of 4'-Fluoro-2'-C-Methyluridine 5'-Phosphoramidate Prodrug (AL-335) for the Treatment of Hepatitis C Infection.
Hepatitis C is a major liver disease caused by hepatitis C virus. Current standard of care for HCV using direct-acting antiviral agents in combination can achieve cure rates above 95%. However, the lo...
The emergence of a deletion mutant at hepatitis C virus (HCV) NS5A-P32 (P32del) has recently been reported in a subset of chronic hepatitis C patients who experience virologic failure after direct-act...
Hepatitis C Virus is constantly evolving genetically, particularly in response to the immune system. This is an observational study to examine if immunosuppressants particularly calcineur...
China is a highly prevalent area of hepatitis B virus（HBV） infection, with at least 75 million hepatitis B virus carriers, and 80% of primary hepatocellular carcinoma (HCC) is associat...
The purpose of the study is to determine if combination therapy with daclatasvir (DCV) and sofosbuvir (SOF) for 8 weeks is safe and effective in patients who have never been treated previo...
The purpose of the study is to investigate the immune response to hepatitis C virus to determine why some people clear the virus and others develop chronic infection. Changes in immune re...
Acute hepatitis C is a liver disease related to a virus: hepatitis C virus (HCV). The type of Hepatitis C Virus present in Egypt (genotype 4), has the reputation to respond poorly to treat...
A family of hepatotropic DNA viruses which contains double-stranded DNA genomes and causes hepatitis in humans and animals. There are two genera: AVIHEPADNAVIRUS and ORTHOHEPADNAVIRUS. Hepadnaviruses include HEPATITIS B VIRUS, duck hepatitis B virus (HEPATITIS B VIRUS, DUCK), heron hepatitis B virus, ground squirrel hepatitis virus, and woodchuck hepatitis B virus (HEPATITIS B VIRUS, WOODCHUCK).
A species in the genus HEPATOVIRUS containing one serotype and two strains: HUMAN HEPATITIS A VIRUS and Simian hepatitis A virus causing hepatitis in humans (HEPATITIS A) and primates, respectively.
A uridine monophosphate analog inhibitor of HEPATITIS C VIRUS (HCV) polymerase NS5B that is used as an ANTIVIRAL AGENT in the treatment of CHRONIC HEPATITIS C.
INFLAMMATION of the LIVER in humans caused by HEPATITIS DELTA VIRUS, a defective RNA virus that can only infect HEPATITIS B patients. For its viral coating, hepatitis delta virus requires the HEPATITIS B SURFACE ANTIGENS produced by these patients. Hepatitis D can occur either concomitantly with (coinfection) or subsequent to (superinfection) hepatitis B infection. Similar to hepatitis B, it is primarily transmitted by parenteral exposure, such as transfusion of contaminated blood or blood products, but can also be transmitted via sexual or intimate personal contact.
A strain of HEPATITIS A VIRUS which causes hepatitis in humans. The virus replicates in hepatocytes and is presumed to reach the intestine via the bile duct. Transmission occurs by the fecal-oral route.
Biological therapy involves the use of living organisms, substances derived from living organisms, or laboratory-produced versions of such substances to treat disease. Some biological therapies for cancer use vaccines or bacteria to stimulate the body&rs...
Astroesophageal Reflux Disease (GERD) Barrett's Esophagus Celiac Disease Cholesterol Crohn's Disease Gastroenterology Hepatitis Hepatology Irritable Bowel Syndrome (IBS) Pancreatitis Peptic Ulcer Disease...
Polymerase Chain Reaction (PCR)
PCR (Polymerase Chain Reaction) uses the ability of DNA polymerase (enzymes that create DNA molecules by assembling nucleotides, the building blocks of DNA. These enzymes are essential to DNA replication and usually work in pairs to create two ident...