For rapid and simultaneous detection of (fluoro)quinolones, a broadly specific monoclonal antibody (mAb) that recognizes 32 (fluoro)quinolone antibiotics was prepared using a mixture of a norfloxacin derivative and a sarfloxacin derivative as the hapten. An immunochromatographic strip based on gold nanoparticles (AuNPs) was then assembled with goat anti-mouse antibody and antigen (sarfloxacin coupled to ovalbumin), used to form the C line and T line, respectively. This antigen competes with the (fluoro)quinolones in a sample incubated with mAbs labeled with AuNPs. The strip can detect 32 (fluoro)quinolones including oxolinic acid, nalidixic acid, miloxacin, pipemidic acid, piromidic acid, rosoxacin, cinoxacin, norfloxacin, pefloxacin, lomfloxacin, enofloxacin, fleroxacin, ciprofloxacin, enrofloxacin, dafloxacin, orbifloxacin, sparfloxacin, gemifloxacin, besifloxacin, balofloxacin, gatifloxacin, moxifloxacin, nadifloxacin, ofloxacin, marbofloxacin, flumequine, pazufloxacin, prulifloxacin, sarafloxacin, difloxacin, trovafloxacin, and tosufloxacin in milk within 10 min with the naked eye. The cut-off values of the strip range from 1 to 100 ng/mL and the limits of detection are 0.1–10 ng/mL. The strip does not cross-react with antibiotics including tetracycline, sulfamethazine, ampicillin, erythromycin, aflatoxin B1, or gentamicin. In short, this immunochromatographic strip is a very useful tool for the primary screening of (fluoro)quinolones in milk.
A series of 1,2‐ and 1,4‐dihydroquinolines has been successfully prepared. The Pd‐catalyzed intramolecular N‐arylation of Z‐enamines, formally prepared by the Horner–Wadsworth–Emmons olefination, proceeded efficiently to furnish the cyclized products. Depending on the cyclization conditions, substituted 1,4‐dihydroquinolines and further isomerized 1,2‐dihydroquinolines were independently obtained in high yields with an excellent control of isomerization of the double bond.
With the continued rise of drug‐resistant bacterial infections coupled with the current discouraging state of the antibiotic pipeline, the need for new antibacterial agents that operate through unique mechanisms compared with conventional antibiotics and work in synergy with other agents is at an all‐time high. We have discovered that gallic acid, a plant‐derived phytochemical, dramatically potentiates the antibacterial activities of several halogenated quinolines (up to 11 800‐fold potentiation against Staphylococcus aureus) against pathogenic bacteria, including drug‐resistant clinical isolates. S. aureus demonstrated the highest sensitivity towards gallic acid–halogenated quinoline combinations, including one halogenated quinoline that demonstrated potentiation of biofilm eradication activity against a methicillin‐resistant S. aureus (MRSA) clinical isolate. During our studies, we also demonstrated that these halogenated quionlines operate through an interesting metal(II) cation‐dependent mechanism and display promising mammalian cytotoxicity. 相似文献
4‐Aryl‐2(1H)‐quinolones were efficiently synthesized via copper‐catalyzed hydroarylation of (o‐aminophenyl)propiolates with arylboronic acid neopentyl glycol esters. The substrate propiolates were prepared from the corresponding silylalkynes with carbon dioxide by Kondo’s carboxylation method using N,N‐dimethylformamide as a solvent. Hydroarylation was performed in the presence of 3 mol% copper(II) acetate in methanol at 28 °C for 12 h and subsequent deprotection using trifluoromethanesulfonic acid (3.0 equiv.) at 65 °C for 2 h in the same pot to afford the desired 4‐aryl‐2(1H)‐quinolones in 39–89% yields.
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