1,1'-(3-methyl-4-phenylthieno[2,3-b]thiophene-2,5-diyl)diethanone as a building block in heterocyclic synthesis. Novel synthesis of some pyrazole and pyrimidine derivatives

A series of new bis(heterocycles) featuring thieno[2,3-b]thiophene rings was synthesized in a combinatorial manner. Intramolecular cyclization of enaminone derivatives with appropriate N-nucleophiles afforded the target compounds. All compounds were characterized by 1H-, 13C-NMR, GCMS, IR, and UV-Vis spectrometry. These compounds represent a new class of sulfur- and nitrogen-containing heterocycles that should also be of interest as new materials.     

Facile One‐Pot Synthesis of 4‐Hydroxy‐2‐methyl‐(2H)‐1,2‐benzothiazine‐3‐sulfonic Acid 1,1‐Dioxide

We report a convenient synthesis of 4‐hydroxy‐2‐methyl‐(2H)‐1,2‐benzothiazine‐3‐sulfonic acid‐1,1‐dioxide (6a) prepared in a novel one‐pot reaction. The synthesis involves two transformations starting from 2‐methyl‐2H‐1,2‐benzothiazin‐4‐(3H)‐one 1,1‐dioxide (7) with an overall yield better than that from the stepwise process, as well as the alternate procedure starting from saccharin (1). One‐pot synthesis of an important intermediate, saccharin‐N‐methane sulfonic acid (4), is also described.     

Mild and Efficient Solvent‐Free Friedel–Crafts Acylation of Reserpine

The first mild, efficient, solvent‐free Friedel–Crafts acylation of reserpine has been developed, which resulted in the synthesis of 10‐ and 12‐acylated homologues in high overall yields.     

Anodic fluorination of 4-methoxy-1-naphthol and 4-nitroanisole using Et3N · 5 HF in mixed nonaqueous solvent

Anodic fluorination of 4-methoxy-1-naphthol and 4-nitroanisole has been investigated in a mixed nonaqueous solvent using Et₃N · 5 HF as supporting electrolyte as well as fluorine source. In order to avoid the formation of polymer on the anode, pulse electrolysis was carried out without exchanging the electrodes. The proposed procedure ensures excellent yield at room temperature, shortest reaction time, and easy work-up which provide additional advantages in the context of green chemistry. Experimental parameters of the reaction are discussed.     

Dye fixation and decolourization of vinyl sulphone reactive dyes by using dicyanidiamide fixer in the presence of ferric chloride

A synthetic polymer was synthesized and used for the improvement of dyeing properties as well as decolorization of textile waste water. Two dyes were selected having anthraquinone based Remazol Blue R and azo based Remazol Red RB. It was observed that the synthetic polymer can be used as fixer for the fixation of dye by crosslinking between dye and fibre, which not only improves the dyeing properties but also helpful to coagulate the colour after dyeing. By single point method the concentrations of synthetic polymer were calculated in residual after dyeing. It was examined that the residual synthetic polymer is helpful in colour removal efficiency by coagulation of polymer with dye to form heavy molecules which settle down and decolorization occurred. Colour removal efficiency was found dependents on pH, concentration of synthetic polymer and inorganic coagulant.     

Phosphorescence properties of sol–gel derived ruby measured as functions of temperature and Cr<Superscript>3+</Superscript> content

A novel approach for the contactless measurement of surface temperatures is to evaluate the temperature dependent phosphorescence properties of chromium doped aluminium oxide (ruby) coatings, such as phosphorescence intensity, spectral distribution, or the phosphorescence lifetime. However, these properties are also affected by the chromium content in the films. In the present study the phosphorescence lifetimes were studied for the first time as a function of the chromium content. We use a simple sol–gel depositing technique for the preparation of precisely doped ruby coatings in Si(100) substrates. These coatings (Cr-to-Al-ratios y between 0% and 6.8 at. %) are well suited for studying the influence of the chromium concentration on the phosphorescence properties: at room temperature (294 K), the phosphorescence intensity is strongly affected by the chromium doping (maximum at y∼1–1.5%) while the spectrum shifts only slightly with varying chromium content. The phosphorescence lifetime τ at 294 K remains constant with varying Cr³⁺ content below y∼1.1%, and decreases strongly above y∼1.1%. Thus, ruby doped with y∼1% seems to be most promising as a temperature sensor because it shows the highest phosphorescence intensity and a low variance in the phosphorescence lifetimes. Due to the latter property the temperature evaluation from τ is less affected by imprecise doping. The phosphorescence lifetimes of several sol–gel ruby coatings (y=1.1%) on Si(100) substrates were measured as a function of the temperature to be between 2.7 ms at 294 K and 4 μs at 833 K. PACS 07.20.Dt; 78.55.-m; 78.66.-w     

Microglial responses around intrinsic CNS neurons are correlated with axonal regeneration

Background  

Microglia/macrophages and lymphocytes (T-cells) accumulate around motor and primary sensory neurons that are regenerating axons but there is little or no microglial activation or T-cell accumulation around axotomised intrinsic CNS neurons, which do not normally regenerate axons. We aimed to establish whether there was an inflammatory response around the perikarya of CNS neurons that were induced to regenerate axons through a peripheral nerve graft.     

MHD natural convective flow through a porous medium in a square cavity filled with liquid gallium

This article contains a computational study of free convective flow through a square enclosure filled with liquid gallium saturated porous medium in the presence of a uniform inclined magnetic field. Lower boundary of enclosure is considered to be heated uniformly, upper horizontal boundary is taken insulated, left wall of the cavity is heated linearly, and right wall is heated linearly or taken cold. Navier–Stokes equations governing the flow problem are first exposed to penalty method to eliminate the pressure terms and then Galerkin FEM is employed to solve reduced equations. Grid independent results are achieved and shown in tabular form for numerous ranges of physical flow parameters. To ensure the accuracy of developed code, computed results are compared with those available in earlier studies through figures. It is found that the strength of streamlines circulation is increased due to increase in Darcy number while imposition of vertical magnetic field instead of horizontal magnetic field causes slow rate of increase in strength of streamlines circulation. Whereas, in the case of linearly heated right wall, the average Nusselt number is an increasing function of the Darcy number, and vertical magnetic field causes higher values for average Nusselt number as compared to horizontal magnetic field along bottom and side walls of cavity. Contrarily, in the case of cold right wall, the horizontal magnetic field results in higher values of average Nusselt number as compared to the vertical magnetic field case, and the average Nusselt number reduces as we move along lower and right boundary while increases along left wall with increase in distance.     

Synthesis and Evaluation of Anti-HIV Activity of Mono- and Di-Substituted Phosphonamidate Conjugates of Tenofovir

The activity of nucleoside and nucleotide analogs as antiviral agents requires phosphorylation by endogenous enzymes. Phosphate-substituted analogs have low bioavailability due to the presence of ionizable negatively-charged groups. To circumvent these limitations, several prodrug approaches have been proposed. Herein, we hypothesized that the conjugation or combination of the lipophilic amide bond with nucleotide-based tenofovir (TFV) (1) could improve the anti-HIV activity. During the current study, the hydroxyl group of phosphonates in TFV was conjugated with the amino group of L-alanine, L-leucine, L-valine, and glycine amino acids and other long fatty ester hydrocarbon chains to synthesize 43 derivatives. Several classes of derivatives were synthesized. The synthesized compounds were characterized by 1H NMR, IR, UV, and mass spectrometry. In addition, several of the synthesized compounds were evaluated as racemic mixtures for anti-HIV activity in vitro in a single round infection assay using TZM-bl cells at 100 ng/mL. TFV (1) was used as a positive control and inhibited HIV infection by 35%. Among all the evaluated compounds, the disubstituted heptanolyl ester alanine phosphonamidate with naphthol oleate (69), pentanolyl ester alanine phosphonamidate with phenol oleate (62), and butanolyl ester alanine phosphonamidate with naphthol oleate (87) ester conjugates of TFV were more potent than parent drug TFV with 79.0%, 76.5%, 71.5% inhibition, respectively, at 100 ng/mL. Furthermore, two fatty acyl amide conjugates of tenofovir alafenamide (TAF) were synthesized and evaluated for comparative studies with TAF and TFV conjugates. Tetradecanoyl TAF conjugate 95 inhibited HIV infection by 99.6% at 100 ng/mL and showed comparable activity to TAF (97–99% inhibition) at 10–100 ng/mL but was more potent than TAF when compared at molar concentration.