Abstract
The Mur ligases have an essential role in the intracellular biosynthesis of bacterial peptidoglycan, and they represent attractive targets for the design of novel antibacterials. A series of compounds with an N-acylhydrazone scaffold were synthesized and screened for inhibition of the MurC and MurD enzymes from Escherichia coli. Compounds with micromolar inhibitory activities against both MurC and MurD were identified, and some of them also showed antibacterial activity.
Publication types
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Research Support, Non-U.S. Gov't
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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Bacterial Proteins / antagonists & inhibitors
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Bacterial Proteins / chemistry
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Crystallography, X-Ray
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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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Hydrazones / chemical synthesis*
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Hydrazones / chemistry
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Hydrazones / pharmacology*
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Ligases / antagonists & inhibitors*
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Ligases / chemistry
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Microbial Sensitivity Tests
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Models, Molecular
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Molecular Structure
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Peptidoglycan / biosynthesis
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Staphylococcus aureus / drug effects
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Stereoisomerism
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Structure-Activity Relationship
Substances
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Anti-Bacterial Agents
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Bacterial Proteins
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Enzyme Inhibitors
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Hydrazones
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Peptidoglycan
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Ligases