Abstract
A series of bridged monocyclic beta-lactams activated by various groups on the beta-lactam nitrogen (X = OCH2CO2H, OSO3H) has been synthesized and evaluated. Among them, the bridged sulfactams (X = OSO3H) were found to be effective beta-lactamase inhibitors. They inhibit both class A and class C beta-lactamases.
MeSH terms
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Acetates / chemical synthesis*
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Acetates / chemistry
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Acetates / pharmacology
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Ceftriaxone / pharmacology
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Cephalosporins / pharmacology
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Citrobacter freundii / drug effects
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Citrobacter freundii / enzymology
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Drug Design*
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Drug Synergism
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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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Escherichia coli / drug effects
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Escherichia coli / enzymology
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Kinetics
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Pseudomonas aeruginosa / drug effects
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Pseudomonas aeruginosa / enzymology
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Sulfonic Acids / chemical synthesis*
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Sulfonic Acids / chemistry
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Sulfonic Acids / pharmacology
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beta-Lactamase Inhibitors*
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beta-Lactams / chemical synthesis*
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beta-Lactams / chemistry
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beta-Lactams / pharmacology
Substances
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Acetates
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Cephalosporins
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Enzyme Inhibitors
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Sulfonic Acids
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beta-Lactamase Inhibitors
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beta-Lactams
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Ceftriaxone