9 research outputs found
2-Acetylpyridine thiocarbonohydrazones. Potent inactivators of herpes simplex virus ribonucleotide reductase
A Ureido-Thioisobutyric Acid (GW9578) Is a Subtype-Selective PPARα Agonist with Potent Lipid-Lowering Activity
The Naphthyridinone GSK364735 Is a Novel, Potent Human Immunodeficiency Virus Type 1 Integrase Inhibitor and Antiretroviral
The Naphthyridinone GSK364735 Is a Novel, Potent Human Immunodeficiency Virus Type 1 Integrase Inhibitor and Antiretroviral
Discovery of a Potent Boronic Acid Derived Inhibitor of the HCV RNA-Dependent RNA Polymerase
Neuromuscular Blocking Activity and Therapeutic Potential of Mixed-Tetrahydroisoquinolinium Halofumarates and Halosuccinates in Rhesus Monkeys
Novel 4,4-Disubstituted Piperidine-Based C–C Chemokine Receptor-5 Inhibitors with High Potency against Human Immunodeficiency Virus-1 and an Improved human Ether-a-go-go Related Gene (hERG) Profile
Discovery of a Potent Boronic Acid Derived Inhibitor of the HCV RNA-Dependent RNA Polymerase
A boronic acid moiety was found to
be a critical pharmacophore for enhanced in vitro potency against
wild-type hepatitis C replicons and known clinical polymorphic and
resistant HCV mutant replicons. The synthesis, optimization, and structure–activity
relationships associated with inhibition of HCV replication in a subgenomic
replication system for a series of non-nucleoside boron-containing
HCV RNA-dependent RNA polymerase (NS5B) inhibitors are described.
A summary of the discovery of <b>3</b> (GSK5852), a molecule
which entered clinical trials in subjects infected with HCV in 2011,
is included