Search Results - "DOERFFLER, Edward"
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Discovery and Synthesis of a Phosphoramidate Prodrug of a Pyrrolo[2,1‑f][triazin-4-amino] Adenine C‑Nucleoside (GS-5734) for the Treatment of Ebola and Emerging Viruses
Published in Journal of medicinal chemistry (09-03-2017)“…The recent Ebola virus (EBOV) outbreak in West Africa was the largest recorded in history with over 28,000 cases, resulting in >11,000 deaths including >500…”
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Early Development and Kilogram Scale-Up of a Non-steroidal FXR Agonist for the Treatment of Non-alcoholic Steatohepatitis (NASH)
Published in Organic process research & development (18-03-2022)“…Non-alcoholic steatohepatitis (NASH) is a serious chronic liver disease characterized by progressive fibrosis that can lead to cirrhosis, liver failure, and…”
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Preclinical Characterization of GS-9669, a Thumb Site II Inhibitor of the Hepatitis C Virus NS5B Polymerase
Published in Antimicrobial Agents and Chemotherapy (01-02-2013)“…Classifications Services AAC Citing Articles Google Scholar PubMed Related Content Social Bookmarking CiteULike Delicious Digg Facebook Google+ Mendeley Reddit…”
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Poly(4-(aminomethyl)styrene)-b-polystyrene: Synthesis and Unilamellar Vesicle Formation
Published in Langmuir (05-03-2002)Get full text
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Therapeutic efficacy of the small molecule GS-5734 against Ebola virus in rhesus monkeys
Published in Nature (London) (17-03-2016)“…The discovery is reported of a small molecule drug, GS-5734, which has antiviral activity against Ebola virus and other filoviruses, and is capable of…”
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The synthesis of 2-ketopiperazine acetic acid esters and amides from ethylenediamines with maleates and maleimides
Published in Tetrahedron letters (24-02-2003)“…The reaction of substituted ethylenediamines with various fumarates, maleates, and maleimides to form substituted ketopiperazine acetic acid esters and amides…”
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Benzyl Acetate and Benzyl Ether Groups as Latent Initiator Sites for Atom Transfer Radical Polymerization
Published in Macromolecules (28-11-2000)Get full text
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Discovery of the First C‑Nucleoside HCV Polymerase Inhibitor (GS-6620) with Demonstrated Antiviral Response in HCV Infected Patients
Published in Journal of medicinal chemistry (13-03-2014)“…Hepatitis C virus (HCV) infection presents an unmet medical need requiring more effective treatment options. Nucleoside inhibitors (NI) of HCV polymerase…”
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Discovery of GS-7682, a Novel 4′-Cyano-Modified C‑Nucleoside Prodrug with Broad Activity against Pneumo- and Picornaviruses and Efficacy in RSV-Infected African Green Monkeys
Published in Journal of medicinal chemistry (08-08-2024)“…Acute respiratory viral infections, such as pneumovirus and respiratory picornavirus infections, exacerbate disease in COPD and asthma patients. A research…”
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Discovery of β-d-2′-deoxy-2′-α-fluoro-4′-α-cyano-5-aza-7,9-dideaza adenosine as a potent nucleoside inhibitor of respiratory syncytial virus with excellent selectivity over mitochondrial RNA and DNA polymerases
Published in Bioorganic & medicinal chemistry letters (15-06-2015)“…[Display omitted] Novel 4′-substituted β-d-2′-deoxy-2′-α-fluoro (2′d2′F) nucleoside inhibitors of respiratory syncytial virus (RSV) are reported. The…”
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Discovery of GS-9669, a Thumb Site II Non-Nucleoside Inhibitor of NS5B for the Treatment of Genotype 1 Chronic Hepatitis C Infection
Published in Journal of medicinal chemistry (13-03-2014)“…Investigation of thiophene-2-carboxylic acid HCV NS5B site II inhibitors, guided by measurement of cell culture medium binding, revealed the structure–activity…”
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Discovery of a 2′-fluoro-2′-C-methyl C-nucleotide HCV polymerase inhibitor and a phosphoramidate prodrug with favorable properties
Published in Bioorganic & medicinal chemistry letters (15-04-2017)“…[Display omitted] A series of 2′-fluorinated C-nucleosides were prepared and tested for anti-HCV activity. Among them, the triphosphate of…”
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Discovery of GS-9256: A novel phosphinic acid derived inhibitor of the hepatitis C virus NS3/4A protease with potent clinical activity
Published in Bioorganic & medicinal chemistry letters (01-02-2012)“…A potent and novel class of phosphinic acid derived product-like inhibitors of the HCV NS3/4A protease was discovered previously. Modification of the…”
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Discovery of GS-9451: An acid inhibitor of the hepatitis C virus NS3/4A protease
Published in Bioorganic & medicinal chemistry letters (01-04-2012)“…The discovery of GS-9451 is reported. Modification of the P3 cap and P2 quinoline with a series of solubilizing groups led to the identification of potent HCV…”
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Discovery of novel phosphonate derivatives as hepatitis C virus NS3 protease inhibitors
Published in Bioorganic & medicinal chemistry letters (01-07-2009)“…The design and preparation of highly potent tricyclic HIV integrase inhibitors are reported. The lead compound has shown good oral bioavailability in both rat…”
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Novel, potent, and orally bioavailable phosphinic acid inhibitors of the hepatitis C virus NS3 protease
Published in Bioorganic & medicinal chemistry letters (15-06-2011)“…A potent and novel class of product-like inhibitors of the HCV NS3 protease was discovered by employing a phosphinic acid as a carboxylate isostere. The…”
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Novel, potent and orally bioavailable indolizidinone-derived inhibitors of the hepatitis C virus NS3 protease
Published in Bioorganic & medicinal chemistry letters (15-01-2012)“…A novel, potent, and orally bioavailable class of product-like inhibitors of the HCV NS3 protease was discovered by constraining the P2–P3 amide bond and the…”
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Optimization of Pharmacokinetics through Manipulation of Physicochemical Properties in a Series of HCV Inhibitors
Published in ACS medicinal chemistry letters (13-10-2011)“…A novel series of HCV replication inhibitors based on a pyrido[3,2-d]pyrimidine core were optimized for pharmacokinetics (PK) in rats. Several associations…”
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