A Novel Approach for the Synthesis of C-Nucleoside Analogs by Constructing Benzoxazine Rings Linked to a Carbohydrate Moiety

Abstract

Dehydrative cyclization of the condensation product of 2, 3, 4, 5-tetra-O-acetyl-galactaryl chloride with anthranilic acid gave 1, 2, 3, 4-tetra-O-acetyl-1, 4-bis(4H-benzoxazin-4-one-2-yl)-galacto-tetritol. Its reaction with aniline in the presence of phosphorus trichloride afforded 1, 4-bis (3-phenylquinazolin-4-one-2-yl)-1, 2, 3, 4-tetra-O-acetyl-galacto-tetritol.     

Synthesis and Rearrangement of Mono and Bis-(p-Fluorophenyl)Hydrazones of Dehydro-L-Ascorbic Acid

Abstract

The mono- and bis-(p-fluorophenyl)hydrazones of dehydro-L-ascorbic acid were prepared. Oxidation of the bis(hydrazone) afforded 3,6-anhydro-3-C-(p-fluorophenylazo) L-xylo-2-hexul osono-1,4-1 actone-2-(p-fluorophenyl)hydrazone. Rearrangement of the bis(hydrazone) gave T-(p-fluorophenyl)-3-(L-threo-glycerol-1-yl)-pyrazoli n-4,5-di one-4-(p-fluorophenyl)hydrazone, whose periodate oxidation gave 3-formyl-1-(p-fluorophenyl pyrazol in-4.5-dione-3-4-(p-fluorophenyl)hydrazone that upon reduction gave 1-(p-fluorophenyl)-3-hydroxymethyl pyrazol in-4,5-dione-4-(p-fluorophenyl)hydrazone. The compounds were characterized as their acetates and benzoates.     

Free vibration multiquadric boundary elements applied to plane elasticity

This paper presents a new boundary element formulation for free vibration analysis of two-dimensional elastic structures. The dual reciprocity method (DRM) is introduced using the multiquadric radial basis functions (MQ). The required particular solution kernels for displacement and traction are derived and smoothed using simple mathematical trick; hence the limiting values of these kernels are computed. The eigen-problem of displacement is formulated and solved to obtain the required frequencies of different vibration modes. Finally, several numerical problems are studied to demonstrate the validity and accuracy of the developed formulation. The results are compared to those obtained from other interpolation functions, and finite element analysis to demonstrate the validity and superiority of the present formulation.     

A new double negative metamaterial for multi-band microwave applications

This paper reveals the design and analysis of a new split-H-shaped metamaterial unit cell structure that is applicable for multi-band frequency range, and it shows negative permeability and permittivity at those frequency bands. In the basic design, the two separate split square resonators have been added by a metal link to form H-shape unit structure. Moreover, the analyses and comparison of the 1 × 1-array, 2 × 2-array structures and 1 × 1, 2 × 2 unit cell configurations have been investigated. All these configurations demonstrate its multi-band operating frequency (S-band, C-band, X-band, K _u -band) with double negative characteristics. The equivalent circuit model for the unit cell is presented to demonstrate the validation of the resonant behavior. The commercially available finite-difference time-domain based simulation software CST microwave studio has been used to get the reflection and transmission parameters of the unit cell. In summation, the material also exhibits single negative characteristics in the multi-band frequency range if it is projected on the 20 × 20 mm² substrates. The simplicity, scalability, double negative characteristics, and multi-band operations have made this design novel in the electromagnetic paradigm.     

Fixed Point Theorems for Monotone Caristi Inward Mappings

In this paper, we introduce the monotone Caristi inward mappings. As an example, we show that monotone inward contraction mappings are monotone Caristi inward mappings. A general fixed point theorem for such mappings is given. A mutlivalued version of these results is also introduced.     

Space‐Confined Seeded Growth of Cu Nanorods with Strong Surface Plasmon Resonance for Photothermal Actuation

Herein, we show that copper nanostructures, if made anisotropic, can exhibit strong surface plasmon resonance comparable to that of gold and silver counterparts in the near‐infrared spectrum. Further, we demonstrate that a robust confined seeded growth strategy allows the production of high‐quality samples with excellent control over their size, morphology, and plasmon resonance frequency. As an example, copper nanorods (CuNRs) are successfully grown in a limited space of preformed rod‐shaped polymer nanocapsules, thereby avoiding the complex nucleation kinetics involved in the conventional synthesis. The method is unique in that it enables the flexible control and fine‐tuning of the aspect ratio and the plasmonic resonance. We also show the high efficiency and stability of the as‐synthesized CuNRs in photothermal conversion and demonstrate their incorporation into nanocomposite polymer films that can be used as active components for constructing light‐responsive actuators and microrobots.     

A modified polyvinylchloride surface with antibacterial and antifouling functions

Surfaces with antibacterial and hydrophilic properties are very attractive to cardiovascular applications. The objective of this study was to synthesize and immobilize a novel antibacterial and hydrophilic polymer onto surface of polyvinylchloride via an effective and mild surface coating technique. The surface coated with a terpolymer constructed with N‐vinylpyrrolidone, 3,4‐dichloro‐5‐hydroxy‐2(5H)‐furanone derivative, and succinimide residue was evaluated with cell adhesion, bacterial adhesion, and bacterial viability. 3T3 mouse fibroblast cells and two bacteria species were used to evaluate surface adhesion and antibacterial activity. Results showed that the polymer‐modified polyvinylchloride surface exhibited not only significantly decreased 3T3 fibroblast cell adhesion with a 66% to 87% reduction but also significantly decreased bacterial adhesion with 69% to 87% and 52% to 74% reduction of Pseudomonas aeruginosa and Staphylococcus aureus attachment, respectively, as compared with original polyvinylchloride. Furthermore, the modified polyvinylchloride surfaces exhibited significant antibacterial functions by inhibiting bacterial growth (75%‐84% and 78–94% inhibition of P aeruginosa and S aureus, respectively, as compared to original polyvinylchloride) and killing bacteria. These results demonstrate that covalent polymer attachment conferred antifouling and antibacterial properties to the polyvinylchloride surface.     

Application of liquid chromatography/thermospray mass spectrometry to studies on the formation of glutathione and cysteine conjugates from monomethylcarbamate metabolites of bambuterol

Liquid chromatography/thermospray mass spectrometry (LC/TSP-MS) has been used to identify and study the rates of formation of S-(N-methylcarbamoyl)cysteine and S-(N-methylcarbamoyl)glutathione as products of the in vitro reaction of cysteine and glutathione, respectively, with two monomethylcarbamate metabolites of the bronchodilator pro-drug bambuterol. The conjugates of interest afforded MH+ species and yielded abundant structurally informative fragment ions which were employed in the development of quantitative, selected-ion monitoring assays. It is concluded that LC/TSP-MS represents a rapid and convenient approach to the direct aqueous-phase analysis of the class of S-(N-alkylcarbamoyl) conjugates of cysteine and glutathione.     

Stability indicating reversed-phase high-performance liquid chromatographic and thin layer densitometric methods for the determination of ziprasidone in bulk powder and in pharmaceutical formulations

Two sensitive and reproducible methods were developed and validated for the determination of ziprasidone (ZIP) in the presence of its degradation products in pure form and in pharmaceutical formulations. The fi rst method was based on reversed-phase high-performance liquid chromatography (HPLC), on a Lichrosorb RP C(18) column using water:acetonitrile:phosphoric acid (76:24:0.5 v/v/v) as the mobile phase at a fl ow rate of 1.5 mL min(-1) at ambient temperature. Quantification was achieved with UV detection at 229 nm over a concentration range of 10-500 micro g mL(-1) with mean percentage recovery of 99.71 +/- 0.55. The method retained its accuracy in presence of up to 90% of ZIP degradation products. The second method was based on TLC separation of ZIP from its degradation products followed by densitometric measurement of the intact drug spot at 247 nm. The separation was carried out on aluminium sheet of silica gel 60 F(254) using choloroform:methanol:glacial acetic acid (75:5:4.5 v/v/v) as the mobile phase, over a concentration range of 1-10 micro g per spot and mean percentage recovery of 99.26 +/- 0.39. Both methods were applied successfully to laboratory prepared mixtures and pharmaceutical capsules.