Novel fluoroquinolones analogues bearing 4-(arylcarbamoyl)benzyl: design, synthesis, and antibacterial evaluation.

Bacterial resistance to fluoroquinolone has been increasing at an alarming rate worldwide. In an attempt to find more potent anti-bacterial agents, an efficient, straightforward protocol was performed to obtain a large substrate scope of novel ciprofloxacin and sarafloxacin analogues conjugated with 4-(arylcarbamoyl)benzyl 7a-ab. All prepared compounds were evaluated for their anti-bacterial activities against three gram-positive strains (Methicillin resistant staphylococcus aureus (MRSA), Staphylococcus aureus, and Enterococcus faecalis) as well as three gram-negative strains (Pseudomonas aeruginosa, Klebsiella pneumonia, and Escherichia coli) through three standard methods including broth microdilution, agar-disc diffusion, and agar-well diffusion assays. Most of the compounds exhibited great to excellent anti-bacterial potencies against MRSA and S. aureus. Among the targeted compounds, derivative 7n exhibited great antibacterial potency, which was noticeably more potent than parent ciprofloxacin. Subsequently, a molecular docking study was performed for this compound to find out its probable binding mode with the active site of S. aureus DNA gyrase (PDB ID: 2XCT).

Synthesis of molecularly imprinted polymer as a nanosorbent for dispersive magnetic micro solid-phase extraction and determination of valsartan in biological samples by UV-Vis Spectrophotometry: Isotherm, kinetics, and thermodynamic studies.

A magnetic molecularly imprinted polymer (MIP) was synthesized by precipitation polymerization utilizing Fe3O4@SiO2-MPS as a magnetic core, itaconic acid as a functional monomer, azobisisobutyronitrile as an initiator, and ethylene glycol dimethacrylate as a cross linker. It was then applied as a nanosorbent for dispersive magnetic micro solid phase extraction (DM-µ-SPE) and determination of valsartan in biological fluids. The morphology and structure of magnetic MIP were characterized by Fourier-transform infrared spectroscopy, Field Emission Scanning electron microscopy, Vibrating sample magnetometer, Energy dispersive x-ray analysis, and Thermogravimetric analysis. The influence of operation conditions on sorption, such as pH (4-10), contact time (10-25 min), initial concentration (1-30 mg L-1), and temperature (25-40 °C) was investigated. After the extraction step, the valsartan concentration was determined by UV-Vis spectrophotometer at 253 nm. The isotherm and kinetic of valsartan sorption were best fitted by the Langmuir model (R2 = 0.987) and the Pseudo second-order kinetic model (R2 = 0.971), respectively. The maximum monolayer sorption capacity for magnetic MIP was obtained to be 4.56 mg g-1. The analytical approach demonstrated favorable figures of merit, with a linear dynamic range of 10-100 µg L-1, a low detection limit of 0.56 µg L-1, and an acceptable preconcentration factor of 5 acquired in optimum conditions. The recoveries of the suggested technique at three spiked levels of analysis were in the range of 101 %-102 %. Valsartan was extracted from various real samples (urine and human blood plasma samples) utilizing the proposed magnetic nanosorbent, and the results exhibited that magnetic MIP was favorable for extraction and measurement of trace amounts of valsartan in biological samples.