一些含三氮杂茂偶氮染料O,N供体的Zr(Ⅱ)配合物的合成、表征和抗微生物活性(英文)

合成了9种3-(2-羟基萘基-1-偶氮)-1,2,4-三氮唑(HL1),3-(2,4-二羟苯基-1-偶氮)-1,2,4-三氮唑(HL2),3-(2-羟基-3-羧基萘基-1-偶氮)-1,2,4-三氮唑(HL3),3-(2-羟基-5-溴苯基-1-偶氮)-1,2,4-三氮唑(HL4)和3-(2-羟基-5-甲基苯基-1-偶氮)-1,2,4-1,2,4-三氮唑(HL5)的Zr(Ⅱ)配合物并用元素分析,摩尔电导,磁矩,IR,UV-Vis,1H-NMR以及热分析(TGA和DTA)对其进行了表征。结果表明HL1-HL5以二齿一元配体方式通过偶氮的氮原子和羟基基团的氧原子与Zr(Ⅱ)离子配位生成单核配合物。用4种革兰氏阴性菌,即大肠杆菌(Escherichia coli),粘质沙雷氏菌(Serratia marcescens),阴沟肠杆菌(Enterobacter cloacae)和普通变形杆菌(Proteus vulgaris),以及2种真菌,即白色念珠菌(Candida albicans)和黑曲霉菌(Aspergillus niger)对配体及其配合物的生物学活性进行了研究。最小抑菌浓度(MICs)用纸上杯碟琼脂扩散法测定,结果表明在大多数情况下,金属化的配合物的抗微生物活性与自由配体相比有所增强。     

Design calculations of an accelerator based BSA for BNCT of brain cancer

Monte Carlo simulations were carried out to calculate optimum design parameters of an accelerator based Beam Shaping Assembly (BSA) for Boron Neutron Capture Therapy (BNCT) of Brain Cancer setup. Epithermal beam of neutrons were obtained through moderation fast neutrons from ⁷Li(p,n) reaction in a high density polyethylene moderator and a graphite reflector. The dimensions of the moderator and the reflector were optimized through optimization of epithermal/fast neutron intensity ratio as a function of geometric parameters of the setup. Results of our calculation showed the capability of our setup to treat the tumor within 4 cm of the head surface. The calculated Peak Therapeutic Ratio for the setup was found to be 2.15. With further improvement in the polyethylene moderator design and brain phantom irradiation-arrangement, the setup capabilities can be improved to reach further deep-seated tumor.     

Simultaneous determination of ofloxacin and ornidazole in pharmaceutical preparations by capillary zone electrophoresis

A simple, rapid and validated capillary electrophoretic method has been developed for the separation and determination of ofloxacin and ornidazole in pharmaceutical formulations with detection at 230 nm. Optimal conditions for the quantitative separations were investigated. Analysis times shorter than 4 min were obtained using a background electrolyte solution consisting of 25 mmol/L phosphoric acid adjusted with 1 m Tris buffer to pH 8.5, with hydrodynamic injection of 5 s and 20 kV separation voltage. The validation criteria for accuracy, precision, linearity and limits of detection and quantitation were examined and discussed. An excellent linearity was obtained in concentration range 25–250 µg/mL. The detection limits for ofloxacin and ornidazole were 1.03 ± 0.11 and 1.80 ± 0.06 µg/mL, respectively. The proposed method has been applied for the analysis of ofloxacin and ornidazole both individually and in a combined dosage tablet formulation. The proposed validated method showed recoveries between 96.16 and 105.23% of the nominal contents. Copyright © 2009 John Wiley & Sons, Ltd.     

Cad for analysis and synthesis of MM-wave transmission lines

This work presents a software for analysis and synthesis of four types of planar lines used on the millimeter wave band: Suspended Microstrip Line, Inverted Microstrip Line, Suspended Stripline and Broadside Coupled Stripline. Conceived for IBM/PG or compatible microcomputers, the program, (MMWL), can study each configuration at a time or all of them at once, and it does not matter if it is synthesis or analysis for each line at the same time. The results are presented in Tables shown in the same screen. The program also provides curves of characteristic impedances against conducting strip width for each one of studied structures. Therefore, it allows choosing the best combination for circuit realization, becoming a helpful tool for projects and with acceptable results.     

Stochastic quantization of the nonlinear sigma model and the background field method

The background field method is a useful scheme for calculation of the effective action in conventional quantum field theory. In stochastic quantization this approach is introduced by using auxiliary fields, as suggested by Okano. In this work, we implement the background field method, using the normal coordinate expansion, for the nonlinear sigma model on a general Riemannian manifold in the context of stochastic quantization. We also calculate, making use of this novel formulation, the action necessary for investigation of the divergences, at least at the one-loop level.     

A Ricci-semi-symmetric hypersurface of Euclidean space which is not semi-symmetric

We construct the first explicit example of a Ricci-semi-symmetric hypersurface of Euclidean space which is not semi-symmetric.

     

Holographic Superconductor of Regular Phantom Black Hole

Holographic superconductors containing a non-minimal derivative coupling for the scalar field in a regular phantom plane symmetric black hole have been considered. We show that the parameter of the regular black hole b as well as the non-minimal derivative coupling parameter η affect the formation of the condensate as well as the conductivity in the superconductor. Moreover, b has a critical value in which the critical temperature T_c increases without a bound.     

Investigation of 3-amino-1,2,4-triazole azodye derivatives as reagents for determination of mercury(II)

The reaction of mercury(II) with 3-(2,4-dihydroxyphen-1-ylazo)-1,2,4-triazole (HL¹), 3-(2-hydroxy-5-methylphen-1-ylazo)-1,2,4-triazole (HL²), 3-(2-hydroxy-5-ethoxycarbonylphen-1-ylazo)-1,2,4-triazole (HL³), 3-(2-hydroxy-5-acetylphen-1-ylazo)-1,2,4-triazole (HL⁴), 3-(2-hydroxy-5-formylphen-1-ylazo)-1,2,4-triazole (HL⁵), and 3-(2-hydroxy-5-bromophen-1-ylazo)-1,2,4-triazole (HL⁶) was studied. A new, direct, and simple procedure was suggested for the spectrophotometric determination of mercury(II) based on its complexation reaction with HL¹-HL⁶. The best reagent was found to be HL³ due to its high sensitivity and selectivity. In aqueous media of pH 9.0 containing 40 vol. % of methanol, Hg(II) reacts with HL³ to form a 1:2 (Hg(II) · HL³) complex having a sensitive absorption peak at 490 nm with the molar extinction coefficient of 3.31 × 10⁴ L mol⁻¹ cm⁻¹ using 4 × 10⁻⁴ M of the reagent. Beer’s law is obeyed over the range from 0.00 μg mL⁻¹ to 12.04 μg mL⁻¹ of mercury(II). The proposed method was applied in the determination of mercury(II) in tap water, seawater and synthetic seawater samples, without the need of prior treatment, with satisfactory results.     

New telluride-mediated elimination for novel synthesis of 2',3'-didehydro-2',3'-dideoxynucleosides

Several 2',3'-dideoxynucleosides (ddNs) and 2',3'-didehydro-2',3'-dideoxynucleosides (d4Ns) are FDA-approved anti-HIV drugs. Via conveniently synthesized 2,2'-anhydronucleosides, we have developed a novel synthesis of d4Ns by discovering and applying a new telluride-mediated elimination reaction. Our experiment results show that after substitution of 2,2'-anhydronucleosides with a telluride monoanion, a telluride intermediate is formed, and its elimination leads to formation of the olefin products (d4Ns). Our mechanistic study indicates that this telluride-assisted reaction consists of two steps: substitution (or addition) and elimination. By using dimethyl ditelluride (0.1 equiv) as the reagent, d4Ns can be synthesized with yields up to 90% via this telluride-mediated elimination. Our novel strategy has great potential to simplify synthesis of these drugs and to further reduce cost of AIDS treatment and will also facilitate development of novel d4N and ddN analogues.     

Synthesis of Pyrazolyl‐Pyrazoles and Pyrazolyl‐[1,2,4]‐Triazolo[3,4‐d][1,5]Benzothiazepines as p53 Activators Using Hydrazonoyl Chlorides

Di‐pyrazoles, tripyrazoles, and pyrazolyltriazolobenzothiazepines were prepared from α,β‐unsaturated ketones and hydrazonoyl chlorides. The structure of all the newly synthesized compounds was established on the bases of their spectral data and elemental analyses. The activity of all products was examined as p53 ubiquitination which showed promising activities.