Journal of Medicinal Chemistry p. 333 - 340 (1987)
Update date:2022-09-26
Topics:
Allen, Norris E.
Alborn, William E.
Kirst, Herbert A.
Toth, John E.
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 strptothricin 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 synthesised 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.
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