Výsledky vyhledávání - "Scott J. Hecker"

Akademický článek

A synthetic lipopeptide targeting top-priority multidrug-resistant Gram-negative pathogens

Publikováno v: Nature Communications, Vol 13, Iss 1, Pp 1-15 (2022)

Polymyxins are often the last therapeutic option for multidrug-resistant (MDR) bacteria, but have suboptimal safety and efficacy. Here the authors report the discovery and development of a synthetic lipopeptide with an improved safety and efficacy ag

Externí odkaz: https://doaj.org/article/0e3e6c3ab9774848b67a0f077533e996

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Scalable On-Demand Production of Purified Diazomethane Suitable for Sensitive Catalytic Reactions

Autor: Anamika Datta, Matthew M. Bio, Changfeng Huang, Scott J. Hecker, Serge H. Boyer, Jillian W. Sheeran, Yuan-Qing Fang, M. Grace Russell, David D. Ford, Kiersten Campbell, Gerald Hummel, Christopher P. Breen

Publikováno v: Organic Process Research & Development. 25:522-528

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% yield. Diazomethane (CH2N2) made with this ...

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::8076cc651bf6101bd3bad5eefab930e2
https://doi.org/10.1021/acs.oprd.0c00485

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Discovery of Cyclic Boronic Acid QPX7728, an Ultrabroad-Spectrum Inhibitor of Serine and Metallo-β-lactamases

Autor: Olga Lomovskaya, Maxim Totrov, Dongxu Sun, K. Raja Reddy, Tomasz W. Glinka, Mojgan Sabet, Debora Rubio-Aparicio, Serge H. Boyer, Orville A. Pemberton, Ruslan Tsivkovski, Scott J. Hecker, Michael N. Dudley, David C. Griffith, Jonathan Parkinson, Kirk Nelson, Yu Chen, Ziad Tarazi

Publikováno v: Journal of Medicinal Chemistry. 63:7491-7507

Despite major advances in the β-lactamase inhibitor field, certain enzymes remain refractory to inhibition by agents recently introduced. Most important among these are the class B (metallo) enzyme NDM-1 of Enterobacteriaceae and the class D (OXA) e

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::0120b5dd24d3ace9b34c3d9db7858b70
https://doi.org/10.1021/acs.jmedchem.9b01976

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Broad-spectrum cyclic boronate β-lactamase inhibitors featuring an intramolecular prodrug for oral bioavailability

Autor: K. Raja Reddy, Maxim Totrov, Olga Lomovskaya, David C. Griffith, Ziad Tarazi, Matthew C. Clifton, Scott J. Hecker

Publikováno v: Bioorganicmedicinal chemistry. 62

Early efforts to broaden the spectrum and potency of cyclic boronic acid β-lactamase inhibitor vaborbactam included a series of 7-membered ring boronates. Exploration of stereoisomers and incorporation of heteroatoms allowed identification of the al

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::10dc909328f0b35fffd16c311436cf23
https://pubmed.ncbi.nlm.nih.gov/35358864

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Selection of QPX7831, an Orally Bioavailable Prodrug of Boronic Acid β-Lactamase Inhibitor QPX7728

Autor: Ziad Tarazi, K. Raja Reddy, Olga Lomovskaya, Jonathan Parkinson, Michael N. Dudley, Serge H. Boyer, Scott J. Hecker, David C. Griffith, Mojgan Sabet

Publikováno v: Journal of medicinal chemistry. 64(23)

In recognition of the need for effective oral therapies to treat Gram-negative bacterial infections, efforts were directed toward identifying an oral prodrug of β-lactamase inhibitor clinical candidate QPX7728. Seventeen prodrugs were synthesized; k

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::43d60110ef6fc895102d041e03ea9e74
https://pubmed.ncbi.nlm.nih.gov/34817182

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QPX7728, An Ultra-Broad-Spectrum B-Lactamase Inhibitor for Intravenous and Oral Therapy: Overview of Biochemical and Microbiological Characteristics

Autor: Scott J. Hecker, Maxim Totrov, Dongxu Sun, Jeffery S. Loutit, Olga Lomovskaya, Raja Reddy, Ruslan Tsivkovski, David A. Griffith, Michael N. Dudley

Publikováno v: Frontiers in Microbiology
Frontiers in Microbiology, Vol 12 (2021)

QPX7728 is a novel β-lactamase inhibitor (BLI) that belongs to a class of cyclic boronates. The first member of this class, vaborbactam, is a BLI in the recently approved Vabomere (meropenem-vaborbactam). In this paper we provide the overview of the

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::56083282633c3ccebe28d9aebab8f1f5
http://europepmc.org/articles/PMC8287861

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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

Autor: Thomas Pabst, Vito LaVopa, Serge H. Boyer, Michel Goldbach, Maria Vasiloiu, André H.M. de Vries, Peter Poechlauer, Christopher Zinganell, Stefan Steinhofer, Peter Hermsen, Ulfried Felfer, Christian Schuster, Scott J. Hecker, Andreas Pelz, Clemens Stueckler, Bas Ritzen, Georg Winkler

Publikováno v: Organic Process Research & Development. 23:1069-1077

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 β-lactamase inhibitor vaborbactam. This includes the successful implementation of the contin

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::d0ac2e33ea6b96ffdc34eaeac6616848
https://doi.org/10.1021/acs.oprd.8b00340

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Cu-Catalyzed Decarboxylative Borylation

Autor: Jie, Wang, Ming, Shang, Helena, Lundberg, Karla S, Feu, Scott J, Hecker, Tian, Qin, Donna G, Blackmond, Phil S, Baran

Publikováno v: ACS Catalysis

A simple method for the conversion of carboxylic acids to boronic esters via redox-active esters (RAEs) is reported using copper catalysis. The scope of this transformation is broad, and compared with the known protocols available, it represents the

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=pmid_dedup__::884feb46dbbcfc7ca873b86633c7e9da
http://europepmc.org/articles/PMC6257631

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