Journal
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
Volume 24, Issue 21, Pages 4943-4947Publisher
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2014.09.037
Keywords
alpha-Hydroxytropolones; Aminoglycoside-2 ''-O-nucleotidyltransferase; Bacterial Resistance; Aminoglycosides; Gentamicin
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Funding
- National Institutes of Health [SC2GM09959]
- Canadian Institutes of Health Research [MT-13536]
- Canada Research Chair program
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Aminoglycoside-2 ''-O-nucleotidyltransferase ANT(2 '')-Ia is an aminoglycoside resistance enzyme prevalent among Gram-negative bacteria, and is one of the most common determinants of enzyme-dependant aminoglycoside-resistance. The following report outlines the use of our recently described oxidopyrylium cycloaddition/ring-opening strategy in the synthesis and profiling of a library of synthetic alpha-hydroxytropolones against ANT(2 '')-Ia. In addition, we show that two of these synthetic constructs are capable of rescuing gentamicin activity against ANT-(2 '')-Ia-expressing bacteria. (C) 2014 Elsevier Ltd. All rights reserved.
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