Abstract
Bridged monobactam beta-lactamase inhibitors were prepared and evaluated as potential partners for combination with imipenem to overcome class C beta-lactamase mediated resistance. The (S)-azepine analog 2 was found to be effective in both in vitro and in vivo assays and was selected for preclinical development.
Copyright (c) 2009 Elsevier Ltd. All rights reserved.
MeSH terms
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Animals
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Bridged Bicyclo Compounds, Heterocyclic / chemistry
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Bridged Bicyclo Compounds, Heterocyclic / pharmacology
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Carbapenems / chemistry*
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Carbapenems / pharmacology
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Drug Combinations
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Drug Discovery / methods*
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Imipenem / chemistry*
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Imipenem / pharmacology
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Mice
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Pseudomonas Infections / drug therapy
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Pseudomonas Infections / enzymology
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Pseudomonas aeruginosa / drug effects
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Pseudomonas aeruginosa / physiology
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Structure-Activity Relationship
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beta-Lactam Resistance / drug effects
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beta-Lactam Resistance / physiology
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beta-Lactamase Inhibitors*
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beta-Lactamases / metabolism
Substances
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Bridged Bicyclo Compounds, Heterocyclic
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Carbapenems
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Drug Combinations
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beta-Lactamase Inhibitors
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Imipenem
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beta-Lactamases