Switch to
Predicate | Object |
---|---|
rdf:type | |
lifeskim:mentions | |
pubmed:issue |
2
|
pubmed:dateCreated |
1987-3-12
|
pubmed:abstractText |
Forty-five aminoglycoside antibiotics and related compounds were compared for their ability to induce the accumulation of dihydrostreptomycin in Escherichia coli K12. The common aminoglycosides and a streptothricin antibiotic all induced enhanced uptake within a relatively narrow concentration range. These concentrations were lethal to the bacteria. Comparison of aminoacyl derivatives of tobramycin and apramycin, the latter synthesized utilizing transition-metal cations to selectively control the site of substitution, revealed that 1-N-aminoacyl modifications resulted in an increased ability to induce enhanced uptake. 2'-N-Aminoacyl modifications were also effective at inducing enhanced uptake, albeit without noticeable improvement over parent. The findings from this structure-activity comparison support the proposition that aminoglycosides share a common critical target (most likely the ribosome), which, when acted upon, results in both drug accumulation and killing.
|
pubmed:language |
eng
|
pubmed:journal | |
pubmed:citationSubset |
IM
|
pubmed:chemical | |
pubmed:status |
MEDLINE
|
pubmed:month |
Feb
|
pubmed:issn |
0022-2623
|
pubmed:author | |
pubmed:issnType |
Print
|
pubmed:volume |
30
|
pubmed:owner |
NLM
|
pubmed:authorsComplete |
Y
|
pubmed:pagination |
333-40
|
pubmed:dateRevised |
2006-11-15
|
pubmed:meshHeading |
pubmed-meshheading:3543366-Aminoglycosides,
pubmed-meshheading:3543366-Anti-Bacterial Agents,
pubmed-meshheading:3543366-Biological Transport,
pubmed-meshheading:3543366-Escherichia coli,
pubmed-meshheading:3543366-Indicators and Reagents,
pubmed-meshheading:3543366-Kinetics,
pubmed-meshheading:3543366-Structure-Activity Relationship
|
pubmed:year |
1987
|
pubmed:articleTitle |
Comparison of aminoglycoside antibiotics with respect to uptake and lethal activity in Escherichia coli.
|
pubmed:publicationType |
Journal Article,
Comparative Study
|