Synthesis and antitumor and antibacterial evaluation of fluoroquinolone derivatives(Ⅲ):Mono- and bis-Schiff-bases

To further explore an efficient modified route for the shift from an antibacterial fluoroquinolone to an antitumor one,mono-Schiff bases 6a-6h related to ciprofloxacin C3 carbonylhydrazone and bis-Schiff bases 4a-4h corresponding to C3/C7 carbonylhydrazone/hydrazone attached on a skeleton of ciprofloquinolone were designed and synthesized,and their in vitro antitumor activity against CHO,HL60,L1210 cells and antibacterial activity against Staphylococcus aureus and Escherichia coli were also reported.     

Improved Synthesis and Structure of 3-Carboxy-2-pyrazinecarbohydroxamic Acid

3-Carboxy-2-pyrazinehydroxamic acid was prepared by a one pot reaction starting from pyrazine-2,3-dicarboxylic anhydride with a high yield, and characterized by IR, Mass spectrum, 1H NMR and 13C NMR spectra and single-crystal X-ray diffraction. It crystallizes in triclinic, space group Pī with a=4.8659(10), b=7.4233(15), c=11.602(2), α=96.904(2), β=92.422(3), γ=107.454(2)°, V=395.51(14)3 , Z=2, Dc=1.689g/cm3 , F(000)=208, μ(MoKα)=0.149 mm-1 , the final R=0.0473 and wR=0.1306 for 2853 observed reflections (I>2σ (I)). A three-dimensional framework was assembled through intermolecular hydrogen bonding between water and 3-carboxy-2-pyrazine-carbohydroxamic acid molecules.     

Effect of solvent on directional drift in Brownian motion of particle/molecule with broken symmetry

The directional drifting of particles/molecules with broken symmetry has received increasing attention. Through molecular dynamics simulations, we investigate the effects of various solvents on the time-dependent directional drifting of a particle with broken symmetry. Our simulations show that the distance of directional drift of the asymmetrical particle is reduced while the ratio of the drift to the mean displacement of the particle is enhanced with increasing mass, size, and interaction strength of the solvent atoms in a short time range. Among the parameters considered, solvent atom size is a particularly influential factor for enhancing the directional drift of asymmetrical particles, while the effects of the interaction strength and the mass of the solvent atoms are relatively weaker. These findings are of great importance to the understanding and control of the Brownian motion of particles in various physical, chemical, and biological processes within finite time spans.     

Development and validation of an LC/MS/MS method for simultaneous determination of shionone and epi‐friedelinol in rat plasma for pharmacokinetic study after oral administration of Aster tataricus extract

A rapid and sensitive liquid chromatography tandem mass spectrometry (LC/MS/MS) method was developed and validated using spinasterol as the internal standard (IS) for the simultaneous determination of shionone and epi‐friedelinol in rat plasma. Plasma samples were pretreated using liquid–liquid extraction with ethyl ether. Chromatographic separation was achieved on a C₁₈ column (100 × 2.1 mm, 5 μm) with an isocratic elution consisting of acetonitrile–0.1% formic acid water (75:25, v/v) at a flow rate of 0.30 mL/min. Detection was performed under the selected reaction monitoring scan using an electrospray ionization in the positive ion mode. The mass transitions were as follows: m/z 427.4 → 95.1 for shionone, m/z 411.4 → 205.2 for epi‐friedelinol and m/z 395.3 → 105.2 for IS. All calibration curves exhibited good linearity (r > 0.995) over the concentration range for both components. The intra‐ and inter‐day precisions at three QC and lower limit of quantitation levels were both <10.21% in terms of relative standard deviation, and the accuracy ranged from ?7.13 to 8.02% in terms of relative error. The extraction recoveries of the compounds ranged from 82.07 to 89.81%. The developed method was successfully applied to the pharmacokinetic study of shionone and epi‐friedelinol after oral administration of Aster tataricus extract to rats. Copyright © 2015 John Wiley & Sons, Ltd.     

Acetate anion-selective encapsulation in the ellipsoidal cavity of symmetrical α,α′,δ,δ′-tetramethyl-cucurbit[6]uril

Four symmetrical α,α′,δ,δ′-tetramethyl-cucurbit[6]uril-based compounds have been prepared and characterised by X-ray crystallography. Their crystal structures displayed the acetate anion-selective encapsulating capability of symmetrical α,α′,δ,δ′-tetramethyl-cucurbit[6]uril. The host–guest interaction between the symmetrical α,α′,δ,δ′-tetramethyl-cucurbit[6]uril and the acetate anion in aqueous solution has also been observed by variable temperature ¹H NMR spectroscopy.     

Convergence of Galerkin truncation for dynamic response of finite beams on nonlinear foundations under a moving load

The present paper investigates the convergence of the Galerkin method for the dynamic response of an elastic beam resting on a nonlinear foundation with viscous damping subjected to a moving concentrated load. It also studies the effect of different boundary conditions and span length on the convergence and dynamic response. A train–track or vehicle–pavement system is modeled as a force moving along a finite length Euler–Bernoulli beam on a nonlinear foundation. Nonlinear foundation is assumed to be cubic. The Galerkin method is utilized in order to discretize the nonlinear partial differential governing equation of the forced vibration. The dynamic response of the beam is obtained via the fourth-order Runge–Kutta method. Three types of the conventional boundary conditions are investigated. The railway tracks on stiff soil foundation running the train and the asphalt pavement on soft soil foundation moving the vehicle are treated as examples. The dependence of the convergence of the Galerkin method on boundary conditions, span length and other system parameters are studied.     

Modeling and optimization of laser transmission joining process between PET and 316L stainless steel using response surface methodology

Laser joining parameters play a very significant role in determining the quality of laser transmission joining between PET films and 316L stainless steel plates. In the present work, Laser power, joining speed and stand-off-distance were considered as joining parameters. The parameters that influence the quality of laser transmission joining were optimized using response methodology for achieving good joint strength and minimal joint width. The central composite second-order Rotational Design (CCRD) has been utilized to plan the experiments and response surface methodology (RSM) is employed to develop mathematical relationships between joining parameters and desired responses. Based on the developed mathematical models, the interaction effects of the process parameters on laser transmission joining were investigated and optimum joining parameters were achieved. The experimental values nearly agree with the predicted values from mathematical models, indicates that the models can predict the responses adequately and optimize the key process parameters quickly.     

ANALOG PREDISTORTION LINEARIZER ON REDUCING CORRECTED AMPLITUDE OVERSHOOT

This paper presents a dual-nonlinear branch linearizer for reducing the corrected amplitude overshoot of conventional single nonlinear branch linearizer. Theoretical analysis is carried out, the analysis is verified by simulation, and a prototype of Ka band 25.28-26.08 GHz dual nonlinear branch linearizer is achieved. It indicates that the corrected amplitude overshoot is less than 0.5 dB, the C/I3 improvement is more than 10 dB related to a single carrier IBO 9 dB, when it is linked and tested for 50 W spacebrone Travelling Wave Tube Amplifier （TWTA）.     

Theoretical analysis of some problems in the measurement of beam divergence angle for EAST neutral beam injector

Beam angular divergence is one of the indicators to evaluate the beam quality. Operating parameters of the beam extraction system could be adjusted to gain better beam quality following the measurement results, which will be helpful not only to study the transmission characteristics of the beam and the power distribution on the heat load components, but also to understand the real-time working condition of the ion source and beam extraction system. This study includes: (1) the theoretical analysis of beam extraction pulse duration for measurement of beam angular divergence; (2) the theoretical analysis of beam intensity distribution during beam transmission for Experimental Advanced Superconducting Tokomak (EAST) neutral beam injector. Those theoretical analyses could point the way to the measurement of beam divergence angle for EAST neutral beam injector.