Abstract
Compound 1, a potent and irreversible inhibitor of β-lactamases, is in clinical trials with β-lactam antibiotics for the treatment of serious and antibiotic-resistant bacterial infections. A short, scalable, and cost-effective route for the production of this densely functionalized polycyclic molecule is described.
MeSH terms
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Anti-Bacterial Agents / chemical synthesis
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Anti-Bacterial Agents / chemistry
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Anti-Bacterial Agents / pharmacology*
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Azabicyclo Compounds / chemical synthesis
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Azabicyclo Compounds / chemistry
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Azabicyclo Compounds / pharmacology*
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Enzyme Inhibitors / chemical synthesis
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Enzyme Inhibitors / chemistry
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Enzyme Inhibitors / pharmacology*
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Molecular Structure
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Polycyclic Compounds / chemical synthesis
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Polycyclic Compounds / chemistry
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Polycyclic Compounds / pharmacology*
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Structure-Activity Relationship
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beta-Lactamase Inhibitors*
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beta-Lactamases / metabolism
Substances
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Anti-Bacterial Agents
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Azabicyclo Compounds
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Enzyme Inhibitors
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Polycyclic Compounds
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beta-Lactamase Inhibitors
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beta-Lactamases
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relebactam