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

Bioorganic & Medicinal Chemistry
2022-05 | Journal article
DOI: 10.1016/j.bmc.2022.116722
Contributors: K. Raja Reddy; Maxim Totrov; Olga Lomovskaya; David C. Griffith; Ziad Tarazi; Matthew C. Clifton; Scott J. Hecker
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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

Organic Process Research & Development
2022-03-18 | Journal article
DOI: 10.1021/acs.oprd.1c00285
Contributors: Serge H. Boyer; Angela Gonzalez-de-Castro; J.A. Hubertus Dielemans; Laurent Lefort; Zuolin Zhu; Matthias Gnahn; Julia Schörghuber; Stefan Steinhofer; André H. M. de Vries; Scott J. Hecker
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Selection of QPX7831, an Orally Bioavailable Prodrug of Boronic Acid β-Lactamase Inhibitor QPX7728

Journal of Medicinal Chemistry
2021-12-09 | Journal article
DOI: 10.1021/acs.jmedchem.1c01722
Contributors: K. Raja Reddy; Jonathan Parkinson; Mojgan Sabet; Ziad Tarazi; Serge H. Boyer; Olga Lomovskaya; David C. Griffith; Scott J. Hecker; Michael N. Dudley
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Scalable On-Demand Production of Purified Diazomethane Suitable for Sensitive Catalytic Reactions

Organic Process Research & Development
2021-03-19 | Journal article
DOI: 10.1021/acs.oprd.0c00485
Contributors: Jillian W. Sheeran; Kiersten Campbell; Christopher P. Breen; Gerald Hummel; Changfeng Huang; Anamika Datta; Serge H. Boyer; Scott J. Hecker; Matthew M. Bio; Yuan-Qing Fang et al.
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Discovery of Cyclic Boronic Acid QPX7728, an Ultrabroad-Spectrum Inhibitor of Serine and Metallo-β-lactamases

Journal of Medicinal Chemistry
2020-07-23 | Journal article
DOI: 10.1021/acs.jmedchem.9b01976
Contributors: Scott J. Hecker; K. Raja Reddy; Olga Lomovskaya; David C. Griffith; Debora Rubio-Aparicio; Kirk Nelson; Ruslan Tsivkovski; Dongxu Sun; Mojgan Sabet; Ziad Tarazi et al.
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