Synthesis and biological evaluation of 5′-O-dicarboxylic fatty acyl monoester derivatives of anti-HIV nucleoside reverse transcriptase inhibitors

A number of 5′-O-dicarboxylic fatty acyl monoester derivatives of 3′-azido-3′-deoxythymidine (zidovudine, AZT), 2′,3′-didehydro-2′,3′-dideoxythymidine (stavudine, d4T), and 3′-fluoro-3′-deoxythymidine (alovudine, FLT) were synthesized to improve the lipophilicity and potentially the cellular delivery of parent polar 2′,3′-dideoxynucleoside (ddN) analogs. The compounds were evaluated for their anti-HIV activity. Three different fatty acids with varying chain length of suberic acid (octanedioic acid), sebacic acid (decanedioic acid), and dodecanedioic acid were used for the conjugation with the nucleosides. The compounds were evaluated for anti-HIV activity and cytotoxicity. All dicarboxylic ester conjugates of nucleosides exhibited significantly higher anti-HIV activity than that of the corresponding parent nucleoside analogs. Among all the tested conjugates, 5′-O-suberate derivative of AZT (EC₅₀ = 0.10 nM) was found to be the most potent compound and showed 80-fold higher anti-HIV activity than AZT without any significant toxicity (TC₅₀ >500 nM).     

Design and synthesis of novel 1,3,4-oxadiazole based azaspirocycles catalyzed by NaI under mild condition and evaluated their antidiabetic and antibacterial activities

A modest, efficient, and mild synthetic procedure has been developed for the synthesis of novel series of 1,3,4-oxadiazole containing azaspirocycles derivatives. The reaction of 1,3,4-oxadiazole derivative with diverse azaspiro compounds under room temperature condition with helps of sodium iodide catalyst and polar aprotic solvent. Numerous compensations of this strategy embrace less time required, yield increment, consumption of all reactants, and mild condition. All synthesized compounds evaluated for in vitro antidiabetic and antibacterial screening. Among them some compounds show significant biological response.     

Electrocatalytic sensing of omeprazole

Ionics - A novel, simple, sensitive, and highly selective omeprazole sensor based on the synergistic effect of polyaniline (PANI) and multiwalled carbon nanotubes (MWCNTs) has been developed. The...     

Microwave-Assisted Graft Copolymerization of Cellulosic Fibers for Removal of Heavy Metal Ions from Aqueous Solution

Functional materials obtained from cellulosic biofibers have gained attention due to the growing demand for them in the field of wastewater remediation. In view of the technological significance of functionalized cellulosic biofibers in wastewater treatment, the present study is a green approach to functionalized cellulosic fibers through graft copolymerization under microwave irradiation. The grafted cellulosic polymers were subsequently subjected to heavy metal ion adsorption studies in order to assess their application in wastewater remediation. The effects of pH, contact time, temperature, and metal ion concentration were studied in batchwise adsorption experiments. The Langmuir, Freundlich, and Tempkin models were used to show the adsorption isotherms. The maximum monolayer capacities, q _m. calculated using the Langmuir isotherm for Zn²⁺, Cd²⁺, and Pb²⁺ were found to be 37.79, 69.68, and 96.81 mg/g respectively. The thermodynamic parameter ΔH° and ΔG° values for metal ion adsorption on functionalized cellulosic fibers showed that adsorption process was spontaneous as well as exothermic in nature.     

A High-Performance Thin-Layer Chromatographic Method for the Evaluation of Marmelosin from Aegle marmelos Corr. Extract and Its Traditional Formulation from Rat Plasma: Application to Pharmacokinetics

JPC – Journal of Planar Chromatography – Modern TLC - Marmelosin is one of the major phytochemical constituents of Aegle marmelos (L.) Corr. (Rutaceae). Till date, there are no methods...     

Structurally Stabilized Organosilane‐Templated Thermostable Mesoporous Titania

Structurally thermostable mesoporous anatase TiO₂ (m‐TiO₂) nanoparticles, uniquely decorated with atomically dispersed SiO₂, is reported for the first time. The inorganic Si portion of the novel organosilane template, used as a mesopores‐directing agent, is found to be incorporated in the pore walls of the titania aggregates, mainly as isolated sites. This is evident by transmission electron microscopy and high‐angle annular dark field scanning transmission electron microscopy, combined with electron dispersive X‐ray spectroscopy. This type of unique structure provides exceptional stability to this new material against thermal collapse of the mesoporous structure, which is reflected in its high surface area (the highest known for anatase titania), even after high‐temperature (550 °C) calcination. Control of crystallite size, pore diameter, and surface area is achieved by varying the molar ratios of the titanium precursor and the template during synthesis. These mesoporous materials retain their porosity and high surface area after template removal and further NaOH/HCl treatment to remove silica. We investigate their performance for dye‐sensitized solar cells (DSSCs) with bilayer TiO₂ electrodes, which are prepared by applying a coating of m‐TiO₂ onto a commercial titania (P25) film. The high surface area of the upper mesoporous layer in the P25–m‐TiO₂ DSSC significantly increases the dye loading ability of the photoanode. The photocurrent and fill factor for the DSSC with the bilayer TiO₂ electrode are greatly improved. The large increase in photocurrent current (ca. 56 %) in the P25–m‐TiO₂ DSSC is believed to play a significant role in achieving a remarkable increase in the photovoltaic efficiency (60 %) of the device, compared to DSSCs with a monolayer of P25 as the electrode.     

Development of 99Mo-alfa-benzoin oxime complex as industrial radiotracer for identification of leaky heat exchanger and its validation with 99mTc

Journal of Radioanalytical and Nuclear Chemistry - In the traditional medicine of Iran, some herbal medicines are used for treating of high blood sugar. In this study, the concentration of Ca, Cr,...     

A quick and regioselective access of spirooxindole-oxazoline by reaction of isatin and isocyanoacetate “on water”

A greener, rapid and regioselective “on water” synthesis of spirooxindole-oxazoline by the reaction of isatin and isocyanoacetate at room temperature is described. The developed protocol has the advantage of being atom-economical, eco-friendly, and benign reaction conditions. Broader substrate scope, experimentally simple procedures, and easy purification of products with high yield further make this method attractive. The synthesized compounds have been fully characterized with spectral analysis.     

Formation and Structure of Fluorescent Silver Nanoclusters at Interfacial Binding Sites Facilitating Oligomerization of DNA Hairpins

Fluorescent, DNA‐stabilized silver nanoclusters (DNA‐AgNCs) are applied in a range of applications within nanoscience and nanotechnology. However, their diverse optical properties, mechanism of formation, and aspects of their composition remain unexplored, making the rational design of nanocluster probes challenging. Herein, a synthetic procedure is described for obtaining a high yield of emissive DNA‐AgNCs with a C‐loop hairpin DNA sequence, with subsequent purification by size‐exclusion chromatography (SEC). Through a combination of optical spectroscopy, gel electrophoresis, inductively coupled plasma mass spectrometry (ICP‐MS), and small‐angle X‐ray scattering (SAXS) in conjunction with the systematic study of various DNA sequences, the low‐resolution structure and mechanism of the formation of AgNCs were investigated. Data indicate that fluorescent DNA‐AgNCs self‐assemble by a head‐to‐head binding of two DNA hairpins, bridged by a silver nanocluster, resulting in the modelling of a dimeric structure harboring an Ag₁₂ cluster.     

A ghost fluid Lattice Boltzmann method for complex geometries

A ghost fluid Lattice Boltzmann method (GF‐LBM) is developed in this study to represent complex boundaries in Lattice Boltzmann simulations of fluid flows. Velocity and density values at the ghost points are extrapolated from the fluid interior and domain boundary via obtaining image points along the boundary normal inside the fluid domain. A general bilinear interpolation algorithm is used to obtain values at image points which are then extrapolated to ghost nodes thus satisfying hydrodynamic boundary conditions. The method ensures no‐penetration and no‐slip conditions at the boundaries. Equilibrium distribution functions at the ghost points are computed using the extrapolated values of the hydrodynamic variables, while non‐equilibrium distribution functions are extrapolated from the interior nodes. The method developed is general, and is capable of prescribing Dirichlet as well as Neumann boundary conditions for pressure and velocity. Consistency and second‐order accuracy of the method are established by running three test problems including cylindrical Couette flow, flow between eccentric rotating cylinders and flow over a cylinder in a confined channel. Copyright © 2011 John Wiley & Sons, Ltd.