Discovery of a Cyclic Boronic Acid β‑Lactamase Inhibitor (RPX7009) with Utility vs Class A Serine Carbapenemases

The increasing dissemination of carbapenemases in Gram-negative bacteria has threatened the clinical usefulness of the β-lactam class of antimicrobials. A program was initiated to discover a new series of serine β-lactamase inhibitors containing a boronic acid pharmacophore, with the goal of finding...

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Veröffentlicht in:	Journal of medicinal chemistry 2015-05, Vol.58 (9), p.3682-3692
Hauptverfasser:	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
Format:	Artikel
Sprache:	eng
Schlagworte:	Animals Anti-Bacterial Agents - chemistry Anti-Bacterial Agents - pharmacokinetics Anti-Bacterial Agents - pharmacology Bacterial Proteins - antagonists & inhibitors beta-Lactamase Inhibitors - chemistry beta-Lactamase Inhibitors - pharmacokinetics beta-Lactamase Inhibitors - pharmacology beta-Lactamases Boronic Acids - chemistry Boronic Acids - pharmacokinetics Boronic Acids - pharmacology Carbapenems - pharmacology Crystallography, X-Ray Drug Resistance, Bacterial Drug Synergism Gram-Negative Bacteria - drug effects Gram-Negative Bacteria - enzymology Gram-Negative Bacteria - isolation & purification Heterocyclic Compounds, 1-Ring - chemistry Heterocyclic Compounds, 1-Ring - pharmacokinetics Heterocyclic Compounds, 1-Ring - pharmacology Mice Microbial Sensitivity Tests Models, Molecular Rats Stereoisomerism Structure-Activity Relationship
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