关键词: Antibiotic resistance detection Chromogenic cephalosporin Nitrocefin analogues β-Lactamase

Mesh : Biocatalysis Cephalosporins / chemical synthesis chemistry metabolism Chemistry Techniques, Synthetic Drug Evaluation, Preclinical Hydrolysis Kinetics beta-Lactamases / metabolism

来  源:   DOI:10.1016/j.ab.2015.06.032   PDF(Sci-hub)

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.
摘要:
暂无翻译
公众号