| Literature DB >> 25283553 |
Danielle R Hirsch1, Georgina Cox2, Michael P D'Erasmo1, Tushar Shakya2, Christine Meck1, Noushad Mohd3, Gerard D Wright2, Ryan P Murelli4.
Abstract
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 α-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.Entities:
Keywords: Aminoglycoside-2″-O-nucleotidyltransferase; Aminoglycosides; Bacterial Resistance; Gentamicin; α-Hydroxytropolones
Mesh:
Substances:
Year: 2014 PMID: 25283553 PMCID: PMC4798002 DOI: 10.1016/j.bmcl.2014.09.037
Source DB: PubMed Journal: Bioorg Med Chem Lett ISSN: 0960-894X Impact factor: 2.823