Abstract
Pulvinones were synthesized (>180) in arrays and evaluated as inhibitors of early stage cell wall biosynthesis enzymes MurA-MurD. Several pulvinones inhibited Mur enzymes with IC(50)'s in the 1-10 microg/mL range and demonstrated antibacterial activity against Gram-positive bacteria including methicillin-resistant Staphyloccus aureus, vancomycin-resistant Enterococcus faecalis, and penicillin-resistant Streptococcus pneumoniae.
MeSH terms
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Anti-Bacterial Agents / pharmacology
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Anti-Infective Agents / pharmacology
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Carboxylic Acids / chemical synthesis*
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Cell Wall / drug effects
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Cell Wall / metabolism
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Drug Resistance, Bacterial
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Enterococcus faecalis / metabolism
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Inhibitory Concentration 50
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Lactones / chemical synthesis*
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Methicillin / pharmacology
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Microbial Sensitivity Tests
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Models, Chemical
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Penicillins / pharmacology
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Staphylococcus aureus / metabolism
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Streptococcus pneumoniae / metabolism*
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Vancomycin / pharmacology
Substances
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Anti-Bacterial Agents
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Anti-Infective Agents
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Carboxylic Acids
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Lactones
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Penicillins
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Vancomycin
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pulvinic acid
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Methicillin