{Reference Type}: Journal Article
{Title}: Assay for drug discovery: Synthesis and testing of nitrocefin analogues for use as β-lactamase substrates.
{Author}: Ghavami A;Labbé G;Brem J;Goodfellow VJ;Marrone L;Tanner CA;King DT;Lam M;Strynadka NC;Pillai DR;Siemann S;Spencer J;Schofield CJ;Dmitrienko GI;
{Journal}: Anal Biochem
{Volume}: 486
{Issue}: 0
{Year}: Oct 2015 1
{Factor}: 3.191
{DOI}: 10.1016/j.ab.2015.06.032
{Abstract}: We report on the synthesis of three nitrocefin analogues and their evaluation as substrates for the detection of β-lactamase activity. These compounds are hydrolyzed by all four Ambler classes of β-lactamases. Kinetic parameters were determined with eight different β-lactamases, including VIM-2, NDM-1, KPC-2, and SPM-1. The compounds do not inhibit the growth of clinically important antibiotic-resistant gram-negative bacteria in vitro. These chromogenic compounds have a distinct absorbance spectrum and turn purple when hydrolyzed by β-lactamases. One of these compounds, UW154, is easier to synthesize from commercial starting materials than nitrocefin and should be significantly less expensive to produce.