Assay for drug discovery: Synthesis and testing of nitrocefin analogues for use as β-lactamase substrates

التفاصيل البيبلوغرافية
العنوان: Assay for drug discovery: Synthesis and testing of nitrocefin analogues for use as β-lactamase substrates
المؤلفون: Laura Marrone, Dylan R. Pillai, Jürgen Brem, Carol A. Tanner, Valerie J. Goodfellow, Stefan Siemann, Ahmad Ghavami, James Spencer, Natalie C. J. Strynadka, Dustin T. King, Geneviève Labbé, Christopher J. Schofield, Melinda Lam, Gary I. Dmitrienko
المصدر: Analytical Biochemistry. 486:75-77
بيانات النشر: Elsevier BV, 2015.
سنة النشر: 2015
مصطلحات موضوعية: medicine.drug_class, Cephalosporin, Drug Evaluation, Preclinical, Biophysics, Chemistry Techniques, Synthetic, Biochemistry, beta-Lactamases, Hydrolysis, medicine, Nitrocefin, Organic chemistry, Molecular Biology, biology, Drug discovery, Chemistry, Cell Biology, biology.organism_classification, Chromogenic Compounds, Combinatorial chemistry, In vitro, Cephalosporins, Kinetics, Biocatalysis, Bacteria
الوصف: 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.
تدمد: 0003-2697
DOI: 10.1016/j.ab.2015.06.032
URL الوصول: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::3a90dfba1097be24f26ad08d8f7fb729
https://doi.org/10.1016/j.ab.2015.06.032
Rights: CLOSED
رقم الانضمام: edsair.doi.dedup.....3a90dfba1097be24f26ad08d8f7fb729
قاعدة البيانات: OpenAIRE
الوصف
تدمد:00032697
DOI:10.1016/j.ab.2015.06.032