Abstract
Since utilization of menaquinone in the electron transport system is a characteristic of Gram-positive organisms, the 1,4-dihydroxy-2-naphthoate prenyltransferase (MenA) inhibitors 1a and 2a act as selective antibacterial agents against organisms such as methicillin-resistant Stapylococcus aureus (MRSA), Staphylococcus epidermidis (MRSE), and Mycobacterium spp. Growth of drug-resistant Gram-positive organisms was sensitive to the MenA inhibitors, indicating that menaquinone synthesis is a valid new drug target in Gram-positive organisms.
Publication types
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Research Support, N.I.H., Extramural
MeSH terms
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Alkyl and Aryl Transferases / antagonists & inhibitors*
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Alkyl and Aryl Transferases / metabolism
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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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Benzophenones / chemical synthesis*
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Benzophenones / chemistry
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Benzophenones / pharmacology
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Gram-Positive Bacteria / drug effects*
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Gram-Positive Bacteria / enzymology
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Methicillin Resistance
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Microbial Sensitivity Tests
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Mycobacterium / drug effects
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Mycobacterium / enzymology
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Naphthols / metabolism*
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Staphylococcus aureus / drug effects
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Staphylococcus aureus / enzymology
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Staphylococcus epidermidis / drug effects
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Staphylococcus epidermidis / enzymology
Substances
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Anti-Bacterial Agents
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Benzophenones
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Naphthols
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allylaminomethanone-A
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phenethylaminomethanone-A
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1,4-dihydroxy-2-naphthoic acid
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Alkyl and Aryl Transferases