Abstract
A series of new phosphinate compounds were designed and synthesized as inhibitors of the d-glutamic acid-adding enzyme (MurD) involved in peptidoglycan biosynthesis. They were tested against the MurD enzyme from Escherichia coli, allowing initial structure-activity relationships to be deduced. Two compounds had IC(50) values near 100 microM and constitute a promising starting point for further development.
Publication types
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Research Support, Non-U.S. Gov't
MeSH terms
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Bacterial Proteins / antagonists & inhibitors*
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Bacterial Proteins / metabolism
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Drug Design
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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 / enzymology
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Molecular Structure
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Peptide Synthases / antagonists & inhibitors*
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Peptide Synthases / metabolism
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Peptidoglycan / biosynthesis
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Peptidoglycan / drug effects
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Phosphinic Acids* / chemical synthesis
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Phosphinic Acids* / chemistry
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Phosphinic Acids* / pharmacology
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Stereoisomerism
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Structure-Activity Relationship
Substances
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Bacterial Proteins
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Enzyme Inhibitors
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Peptidoglycan
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Phosphinic Acids
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Peptide Synthases
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UDP-N-acetylmuramoylalanine-D-glutamate ligase