Search Results - "Boyer, Serge"

Discovery of Cyclic Boronic Acid QPX7728, an Ultrabroad-Spectrum Inhibitor of Serine and Metallo-β-lactamases by Hecker, Scott J, Reddy, K. Raja, Lomovskaya, Olga, Griffith, David C, Rubio-Aparicio, Debora, Nelson, Kirk, Tsivkovski, Ruslan, Sun, Dongxu, Sabet, Mojgan, Tarazi, Ziad, Parkinson, Jonathan, Totrov, Maxim, Boyer, Serge H, Glinka, Tomasz W, Pemberton, Orville A, Chen, Yu, Dudley, Michael N

“…Despite major advances in the β-lactamase inhibitor field, certain enzymes remain refractory to inhibition by agents recently introduced. Most important among…”
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Discovery of a Cyclic Boronic Acid β‑Lactamase Inhibitor (RPX7009) with Utility vs Class A Serine Carbapenemases by Hecker, Scott J, Reddy, K. Raja, Totrov, Maxim, Hirst, Gavin C, Lomovskaya, Olga, Griffith, David C, King, Paula, Tsivkovski, Ruslan, Sun, Dongxu, Sabet, Mojgan, Tarazi, Ziad, Clifton, Matthew C, Atkins, Kateri, Raymond, Amy, Potts, Kristy T, Abendroth, Jan, Boyer, Serge H, Loutit, Jeffrey S, Morgan, Elizabeth E, Durso, Stephanie, Dudley, Michael N

“…The increasing dissemination of carbapenemases in Gram-negative bacteria has threatened the clinical usefulness of the β-lactam class of antimicrobials. A…”
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Selection of QPX7831, an Orally Bioavailable Prodrug of Boronic Acid β‑Lactamase Inhibitor QPX7728 by Reddy, K. Raja, Parkinson, Jonathan, Sabet, Mojgan, Tarazi, Ziad, Boyer, Serge H, Lomovskaya, Olga, Griffith, David C, Hecker, Scott J, Dudley, Michael N

“…In recognition of the need for effective oral therapies to treat Gram-negative bacterial infections, efforts were directed toward identifying an oral prodrug…”
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Scalable Synthesis of β‑Lactamase Inhibitor QPX7728 by Sequential Nickel-Catalyzed Boron Insertion into a Benzofuran Substrate and Enantioselective Cyclopropanation of the Resulting Vinylboronate by Boyer, Serge H, Gonzalez-de-Castro, Angela, Dielemans, J.A. Hubertus, Lefort, Laurent, Zhu, Zuolin, Gnahn, Matthias, Schörghuber, Julia, Steinhofer, Stefan, de Vries, André H. M, Hecker, Scott J

“…We report the scalable, high-yielding, and highly selective synthesis of the β-lactamase inhibitor QPX7728 featuring two key synthetic steps: nickel-catalyzed…”
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Development of a Continuous Flow Process for a Matteson Reaction: From Lab Scale to Full-Scale Production of a Pharmaceutical Intermediate by Stueckler, Clemens, Hermsen, Peter, Ritzen, Bas, Vasiloiu, Maria, Poechlauer, Peter, Steinhofer, Stefan, Pelz, Andreas, Zinganell, Christopher, Felfer, Ulfried, Boyer, Serge, Goldbach, Michel, de Vries, André, Pabst, Thomas, Winkler, Georg, LaVopa, Vito, Hecker, Scott, Schuster, Christian

“…Within this paper, we present the design, development, and scale-up of a process for a continuous Matteson reaction to produce a key intermediate toward the…”
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Targeting thyroid hormone receptor-β agonists to the liver reduces cholesterol and triglycerides and improves the therapeutic index by Erion, Mark D, Cable, Edward E, Ito, Bruce R, Jiang, Hongjian, Fujitaki, James M, Finn, Patricia D, Zhang, Bao-Hong, Hou, Jinzhao, Boyer, Serge H, van Poelje, Paul D, Linemeyer, David L

“…Despite efforts spanning four decades, the therapeutic potential of thyroid hormone receptor (TR) agonists as lipid-lowering and anti-obesity agents remains…”
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Scalable On-Demand Production of Purified Diazomethane Suitable for Sensitive Catalytic Reactions by Sheeran, Jillian W, Campbell, Kiersten, Breen, Christopher P, Hummel, Gerald, Huang, Changfeng, Datta, Anamika, Boyer, Serge H, Hecker, Scott J, Bio, Matthew M, Fang, Yuan-Qing, Ford, David D, Russell, M. Grace

“…We have developed a convenient development-scale reactor (0.44 mol/h) to prepare diazomethane from N-methyl-N-nitroso-p-toluenesulfonamide (MNTS) in ∼80%…”
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Pradefovir: A Prodrug That Targets Adefovir to the Liver for the Treatment of Hepatitis B by Reddy, K. Raja, Matelich, Michael C, Ugarkar, Bheemarao G, Gómez-Galeno, Jorge E, DaRe, Jay, Ollis, Kristin, Sun, Zhili, Craigo, William, Colby, Timothy J, Fujitaki, James M, Boyer, Serge H, van Poelje, Paul D, Erion, Mark D

“…Adefovir dipivoxil, a marketed drug for the treatment of hepatitis B, is dosed at submaximally efficacious doses because of renal toxicity. In an effort to…”
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Antiviral Efficacy upon Administration of a HepDirect Prodrug of 2′-C-Methylcytidine to Hepatitis C Virus-Infected Chimpanzees by CARROLL, Steven S, KOEPLINGER, Kenneth, FUJITAKI, James M, BOYER, Serge H, LINEMEYER, David L, HECKER, Scott J, ERION, Mark D, VAVREK, Marissa, NANYAN RENA ZHANG, HANDT, Laurence, MACCOSS, Malcolm, OLSEN, David B, RAJA REDDY, K, ZHILI SUN, VAN POELJE, Paul D

“…Classifications Services AAC Citing Articles Google Scholar PubMed Related Content Social Bookmarking CiteULike Delicious Digg Facebook Google+ Mendeley Reddit…”
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A Potent and Selective AMPK Activator That Inhibits de Novo Lipogenesis by Gómez-Galeno, Jorge E, Dang, Qun, Nguyen, Thanh H, Boyer, Serge H, Grote, Matthew P, Sun, Zhili, Chen, Mingwei, Craigo, William A, van Poelje, Paul D, MacKenna, Deidre A, Cable, Edward E, Rolzin, Paul A, Finn, Patricia D, Chi, Bert, Linemeyer, David L, Hecker, Scott J, Erion, Mark D

“…AMP-activated protein kinase (AMPK) is a heterotrimeric kinase that regulates cellular energy metabolism by affecting energy-consuming pathways such as de novo…”
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Synthesis and Biological Evaluation of a Series of Liver-Selective Phosphonic Acid Thyroid Hormone Receptor Agonists and Their Prodrugs by Boyer, Serge H, Jiang, Hongjian, Jacintho, Jason D, Reddy, Mali Venkat, Li, Haiqing, Li, Wenyu, Godwin, Jennifer L, Schulz, William G, Cable, Edward E, Hou, Jinzhao, Wu, Rongrong, Fujitaki, James M, Hecker, Scott J, Erion, Mark D

“…Phosphonic acid (PA) thyroid hormone receptor (TR) agonists were synthesized to exploit the poor distribution of PA-based drugs to extrahepatic tissues and…”
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Synthesis and Characterization of a Novel Liver-Targeted Prodrug of Cytosine-1-β-d-arabinofuranoside Monophosphate for the Treatment of Hepatocellular Carcinoma by Boyer, Serge H, Sun, Zhili, Jiang, Hongjian, Esterbrook, Julie, Gómez-Galeno, Jorge E, Craigo, William, Reddy, K. Raja, Ugarkar, Bheemarao G, MacKenna, Deidre A, Erion, Mark D

“…Cytotoxic nucleosides have proven to be ineffective for the treatment of hepatocellular carcinoma (HCC) due, in part, to their inadequate conversion to their…”
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Liver-Targeted Prodrugs of 2‘-C-Methyladenosine for Therapy of Hepatitis C Virus Infection by Hecker, Scott J, Reddy, K. Raja, van Poelje, Paul D, Sun, Zhili, Huang, Wenjian, Varkhedkar, Vaibhav, Reddy, M. Venkat, Fujitaki, James M, Olsen, David B, Koeplinger, Kenneth A, Boyer, Serge H, Linemeyer, David L, MacCoss, Malcolm, Erion, Mark D

“…2‘-C-Methyladenosine exhibits impressive inhibitory activity in the cell-based hepatitis C virus (HCV) subgenomic replicon assay, by virtue of intracellular…”
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Delivery of high levels of anti-proliferative nucleoside triphosphates to CYP3A-expressing cells as a potential treatment for hepatocellular carcinoma by MacKenna, Deidre A, Montag, Annika, Boyer, Serge H, Linemeyer, David L, Erion, Mark D

“…Purpose Hepatocellular carcinoma (HCC) is a life-threatening condition with only one drug treatment regimen approved for use. Oncolytic nucleosides are…”
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Adenosine Kinase Inhibitors. 5. Synthesis, Enzyme Inhibition, and Analgesic Activity of Diaryl-erythro-furanosyltubercidin Analogues by Boyer, Serge H, Ugarkar, Bheemarao G, Solbach, Joel, Kopcho, Joseph, Matelich, Michael C, Ollis, Kristin, Gomez-Galeno, Jorge E, Mendonca, Rohan, Tsuchiya, Megumi, Nagahisa, Atsushi, Nakane, Masami, Wiesner, James B, Erion, Mark D

“…Adenosine is an endogenous neuromodulator that when produced in the central and the peripheral nervous systems has anticonvulsant, anti-inflammatory, and…”
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Design, Synthesis, and Characterization of a Series of Cytochrome P450 3A-Activated Prodrugs (HepDirect Prodrugs) Useful for Targeting Phosph(on)ate-Based Drugs to the Liver by Erion, Mark D, Reddy, K. Raja, Boyer, Serge H, Matelich, Michael C, Gomez-Galeno, Jorge, Lemus, Robert H, Ugarkar, Bheemarao G, Colby, Timothy J, Schanzer, Jürgen, van Poelje, Paul D

“…A new class of phosphate and phosphonate prodrugs, called HepDirect prodrugs, is described that combines properties of rapid liver cleavage with high plasma…”
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Stereoselective synthesis of 4- C-methyl-2,3,5-tri- O-benzyl- d-ribofuranose and 4- C-methyl-2,3,5-tri- O-benzyl- l-lyxofuranose by Boyer, Serge H, Ugarkar, Bheemarao G, Erion, Mark D

“…Sugar intermediates 4- C-methyl-2,3,5-tri- O-benzyl- d-ribofuranose ( 8b ) and 4- C-methyl-2,3,5-tri- O-benzyl- l-lyxofuranose ( 8a ) were synthesized by…”
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Specific Inhibition of Formation of Transcription Complexes by a Calicheamicin Oligosaccharide: A Paradigm for the Development of Transcriptional Antagonists by Ho, Steffan N., Boyer, Serge H., Schreiber, Stuart L., Danishefsky, Samuel J., Crabtree, Gerald R.

“…Sequence-specific DNA ligands that antagonize DNA-protein interactions represent a potentially powerful means of modulating gene expression. Calicheamicin γ1…”
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Studies Related to the Carbohydrate Sectors of Esperamicin and Calicheamicin: Definition of the Stability Limits of the Esperamicin Domain and Fashioning of a Glycosyl Donor from the Calicheamicin Domain by Halcomb, Randall L, Boyer, Serge H, Wittman, Mark D, Olson, Steven H, Denhart, Derek J, Liu, Kevin K. C, Danishefsky, Samuel J

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Interaction of calicheamicin γ1I and its related carbohydrates with DNA–protein complexes by Sissi, Claudia, Aiyar, Jayshree, Boyer, Serge, Depew, Kris, Danishefsky, Samuel, Crothers, Donald M.

“…We report studies of the contribution of DNA structure, holding the sequence constant, to the affinity of calicheamicin γ 1 I and its aryltetrasaccharide…”
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