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rdf:type |
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lifeskim:mentions |
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pubmed:issue |
5
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pubmed:dateCreated |
2008-3-10
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pubmed:abstractText |
Several 2-aminotetralones were identified as novel inhibitors of the bacterial enzymes MurA and MurZ. A number of these inhibitors demonstrated antibacterial activity against Staphylococcus aureus and Escherichia coli with MICs in the range 8-128 microg/ml. Based on structure-activity relationships we propose that the alpha-aminoketone functionality is responsible for the inhibitory activity and evidence is provided to support a covalent mode of action involving the C115 thiol group of MurA/MurZ.
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pubmed:language |
eng
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pubmed:journal |
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pubmed:citationSubset |
IM
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pubmed:chemical |
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pubmed:status |
MEDLINE
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pubmed:month |
Mar
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pubmed:issn |
1464-3405
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pubmed:author |
pubmed-author:AngelesJoseph De LosJde L,
pubmed-author:BlakeKaty LKL,
pubmed-author:ChopraIanI,
pubmed-author:DunsmoreColin JCJ,
pubmed-author:FishwickColin W GCW,
pubmed-author:GarnettJames AJA,
pubmed-author:HendersonPeter J FPJ,
pubmed-author:LeedsJennifer AJA,
pubmed-author:MillerKeithK,
pubmed-author:PalestrantDeborah JDJ,
pubmed-author:PatchingSimon GSG,
pubmed-author:PhillipsSimon E VSE,
pubmed-author:StubbingsWilliam JWJ
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pubmed:issnType |
Electronic
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pubmed:day |
1
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pubmed:volume |
18
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pubmed:owner |
NLM
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pubmed:authorsComplete |
Y
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pubmed:pagination |
1730-4
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pubmed:meshHeading |
pubmed-meshheading:18261901-Anti-Bacterial Agents,
pubmed-meshheading:18261901-Bacterial Proteins,
pubmed-meshheading:18261901-Binding Sites,
pubmed-meshheading:18261901-Escherichia coli,
pubmed-meshheading:18261901-Microbial Sensitivity Tests,
pubmed-meshheading:18261901-Models, Molecular,
pubmed-meshheading:18261901-Molecular Structure,
pubmed-meshheading:18261901-Staphylococcus aureus,
pubmed-meshheading:18261901-Structure-Activity Relationship,
pubmed-meshheading:18261901-Tetralones
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pubmed:year |
2008
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pubmed:articleTitle |
2-Aminotetralones: novel inhibitors of MurA and MurZ.
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pubmed:affiliation |
School of Chemistry and Antimicrobial Research Centre, University of Leeds, Leeds LS2 9JT, UK.
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pubmed:publicationType |
Journal Article
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