Inhibition of aminoglycoside-deactivating enzymes APH(3')-IIIa and AAC(6')-Ii by amphiphilic paromomycin O2''-ether analogues

ChemMedChem. 2011 Nov 4;6(11):1961-6. doi: 10.1002/cmdc.201100346. Epub 2011 Sep 8.

Abstract

Novel amphiphilic aminoglycosides are shown to inhibit clinically relevant deactivating enzymes, without undergoing significant deactivation themselves.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Acetyltransferases / antagonists & inhibitors
  • Acinetobacter baumannii / drug effects
  • Amikacin / metabolism
  • Aminoglycosides / chemistry
  • Aminoglycosides / pharmacology
  • Anti-Bacterial Agents / chemistry*
  • Anti-Bacterial Agents / pharmacology*
  • Crystallography, X-Ray
  • Enzyme Inhibitors / pharmacology*
  • Escherichia coli / drug effects
  • Kanamycin Kinase / antagonists & inhibitors*
  • Klebsiella pneumoniae / drug effects
  • Microbial Sensitivity Tests
  • Molecular Structure
  • Paromomycin / analogs & derivatives*
  • Ribosomes / drug effects
  • Ribosomes / metabolism
  • Staphylococcus aureus / drug effects

Substances

  • Aminoglycosides
  • Anti-Bacterial Agents
  • Enzyme Inhibitors
  • Paromomycin
  • Amikacin
  • Acetyltransferases
  • aminoglycoside N(6')-acetyltransferase
  • Kanamycin Kinase

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