aminoglycoside antibiotic activity by synthetic a-hydroxytropolones

Aminoglycoside-2 00 -O-nucleotidyltransferase ANT(2 00 )-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 a-hydroxytropolones against ANT(2 00 )-Ia. In addition, we show that two of these synthetic constructs are capable of