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BioAssay: AID 223430

In vitro antibacterial activity against isoleucyl-tRNA synthetase from Staphylococcus aureus Oxford

A series of beta-diketone acrylate bioisosteres 4 of pseudomonic acid A 1 have been synthesized and evaluated for their ability to inhibit bacterial isoleucyl-tRNA synthetase and act as antibacterial agents. A number of analogues have excellent antibacterial activity. Selected examples were shown to afford good blood levels and to be effective in a murine infection model. ..more
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 Tested Compounds
 Tested Compounds
All(4)
 
 
Unspecified(4)
 
 
 Tested Substances
 Tested Substances
All(4)
 
 
Unspecified(4)
 
 
 Related BioAssays
 Related BioAssays
AID: 223430
Data Source: ChEMBL (220776)
Depositor Category: Literature, Extracted
BioAssay Version:
Deposit Date: 2010-05-20
Modify Date: 2014-08-24

Data Table ( Complete ):           View All Data
Target
Sequence: RecName: Full=Isoleucine--tRNA ligase; AltName: Full=Isoleucyl-tRNA synthetase; Short=IleRS
Description ..   
Protein Family: catalytic core domain of isoleucyl-tRNA synthetases
Comment ..   

Related Protein 3D Structures     More BioActivity Data..
Tested Compounds:
Description:
Title: Synthesis and antibacterial properties of beta-diketone acrylate bioisosteres of pseudomonic acid A.

Abstract: A series of beta-diketone acrylate bioisosteres 4 of pseudomonic acid A 1 have been synthesized and evaluated for their ability to inhibit bacterial isoleucyl-tRNA synthetase and act as antibacterial agents. A number of analogues have excellent antibacterial activity. Selected examples were shown to afford good blood levels and to be effective in a murine infection model.
(PMID: 10406653)
Categorized Comment - additional comments and annotations
From BioAssay Depositor:
Assay Type: Functional
Target Type: Target is a single protein chain
Assay Data Source: Scientific Literature
Protein Target Class: enzyme ligase
Result Definitions
TIDNameDescriptionHistogramTypeUnit
OutcomeThe BioAssay activity outcomeOutcome
1MIC activity commentMIC activity commentString
2MIC standard flagMIC standard flagInteger
3MIC qualifierMIC qualifierString
4MIC published valueMIC published valueFloatug ml-1
5MIC standard valueMIC standard valueFloatug.mL-1

Data Table (Concise)
Data Table ( Complete ):     View All Data
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