Ellipsometric investigations of Fe3+-doped polyvinyl alcohol films

In this work, we study the inclusion mechanism of Fe³⁺ ions in a polyvinyl alcohol (PVA) matrix. Thin films of pure and FeCl₃-doped PVA on silicon substrates, prepared by the spin-coating method, are investigated using spectroscopic ellipsometry (SE) and Fourier transform infrared (FT-IR) spectroscopy. SE measurements of PVA and Fe³⁺-doped thin films are carried out at an incidence angle of 75° over the wavelength range of 0.24–1.1 μm. An optical model is used to obtain the refractive index (n) and the extinction coefficient (k). The gap energy E _g is afterwards evaluated. The Fe³⁺ doping is found to affect strongly the optical parameters of the polymer films. In fact, an increase in the refractive index with doping is observed, resulting from the intermolecular hydrogen bonding between Fe³⁺ ions with the adjacent OH group of PVA. The increase of the thin films' absorption with doping is estimated by the k spectral profile analysis. The gap energy is then calculated and shows an important decrease with the Fe³⁺ filling, more pronounced for low doped samples. Such a behavior is confirmed by FT-IR analysis.     

Synthesis and Anti-Inflammatory Activities of Some Novel S-Pyridyl Glycosides Derivatives

A series of some new acetylated S-glycosides of pyridine-2-thione derivatives, including D-glucose, D-galactose, D-xylose and L-arabinose derivatives were synthesized. Oxidation of some formed S-glycosides derivatives with H₂O₂ afforded the corresponding sulfones. S-Alkylation of pyridine-2-thione derivatives was performed to furnish the S-acyclo deazauridine derivatives. The entire tested compound showed potent anti-inflammatory activity were potent against edema and in the same time inhibited the prostaglandine formation. It is work mention that all the tested compounds showed high safety margin. The structures of the new synthesized compounds have been proved by IR, ¹ HNMR, mass spectra and elemental analysis.     

Gamma induced changes in Makrofol/CdSe nanocomposite films

We applied an ex-situ casting procedure to prepare a nanocomposite (NCP) from Makrofol polycarbonate (PC) and CdSe nanoparticles. The CdSe nanoparticles were prepared by a thermolysis procedure in the presence of N₂ gas flow. Rietveld refinement of x-ray data illustrated that the CdSe adopts a cubic zinc blend structure of 6.057 Å lattice parameter and 2 nm typical grain size. Samples from the prepared NCP were exposed to γ dosages (20 kGy-250 kGy). The modifications induced in the NCP films owing to γ dosages have been studied. The γ irradiation (50 kGy-250 kGy) causes crosslinks that reduce the optical bandgap from 4.15 eV to 3.81 eV, associated with an increase in dielectric parameters and refractive index. This is attributed to an increase in the mass fraction of the disordered regions as specified by x-ray diffraction. The PC-CdSe NCP was found to have a reaction to color modification which makes it suitable for saleable reproduction on a printing press.     

Design,Docking, and Synthesis of Some New Pyrazoline and Pyranopyrazole Derivatives as Anti‐inflammatory Agents

Design and synthesis of some novel pyrazoline and pyranopyrazole derivatives as potential anti‐inflammatory agents are described. Most of the compounds were tested for their anti‐inflammatory (in vitro and in vivo) and ulcerogenic activities. In all tested compounds, it was found that pyrazolines, 2a , and pyrazolopyrano[2,3‐d]pyrimidine 9 are the potent anti‐inflammatory and selective cyclooxygenase‐2 (COX‐2) inhibitor. All compounds are mainly in the safe level. Docking study of 2a and 9 revealed higher affinity for binding with the active site of COX‐2 enzyme like SC‐558, a selective COX‐2 inhibitor.     

Synthesis,characterization and pharmacological investigations of some novel heterocyclic derivatives incorporating pyrene and sugar moieties

A series of substituted pyrene derivatives 2–15 incorporated heterocyclic and sugar moieties were synthesized and evaluated as antiviral activities using 1-acetylpyrene as a starting material. The structure assignment of the new compounds was based on chemical and spectroscopic evidence. The detailed synthesis, spectroscopic data and pharmacological activities of the synthesized compounds were reported.     

Metal- and Catalyst-Free Synthesis of 2-Substituted-Phthalimides Using 2-(Arenesulfonyl)Phthalimide as Key Reagents

Phthalimide derivatives are important in medicinal chemistry, several phthalimidation methodologies have been developed. Here, we report a facile, metal-free, and catalyst-free method for the preparation of N-phthalimides in good to excellent yield by reacting 2-(arenesulfonyl)phthalimides with various amine substrates.     

Jump of a domain and spectrally balanced domains

Let R be a locally finite-dimensional (LFD) integral domain. We investigate two invariants ${j_R(a)={{\rm inf}}\{{\rm height}P-{\rm height} Q\}}$ , where P and Q range over prime ideals of R such that ${Q\subset aR\subseteq P}$ , and ${j(R)={\rm sup}\{j_R(a)\}}$ (called the jump of R), where a range over nonzero nonunit elements of R. We study the jump of polynomial ring and power series ring, we give many results involving jump, and specially we give more interest to LFD-domain R such that j(R)?=?1. We prove that if R is a finite-dimensional divided domain, then R is a Jaffard domain if and only if for all integer ${n,\,j(R[x_1,\ldots,x_n])=1}$ .     

Antifungal Activity of Soft Tissue Extract from the Garden Snail Helix aspersa (Gastropoda,Mollusca)

Gastropods comprise approximately 80% of molluscans, of which land snails are used variably as food and traditional medicines due to their high protein content. Moreover, different components from land snails exhibit antimicrobial activities. In this study, we evaluated the antifungal activity of soft tissue extracts from Helix aspersa against Candida albicans, Aspergillus flavus, and Aspergillus brasiliensis by identifying extract components using liquid chromatography-tandem mass spectrometry (LC-MS-MS). Two concentrations of three extracts (methanol, acetone, and acetic acid) showed antifungal activity. Both acetone (1 g/3 mL) and acetic acid extracts (1 g/mL) significantly inhibited C. albicans growth (p = 0.0001, 5.2 ± 0.2 mm and p = 0.02, 69.7 ± 0.6 mm, respectively). A. flavus and A. brasiliensis growth were inhibited by all extracts at 1 g/mL, while inhibition was observed for acetic acid extracts against A. brasiliensis (p = 0.02, 50.3 ± 3.5 mm). The highest growth inhibition was observed for A. flavus using acetic acid and acetone extracts (inhibition zones = 38 ± 1.7 mm and 3.1 ± 0.7 mm, respectively). LC-MS-MS studies on methanol and acetone extracts identified 11-α-acetoxyprogesterone with a parent mass of 372.50800 m/z and 287.43500 m/z for luteolin. Methanol extracts contained hesperidin with a parent mass of 611.25400 m/z, whereas linoleic acid and genistein (parent mass = 280.4 and 271.48900 m/z, respectively) were the main metabolites.     

Discovery of New VEGFR-2 Inhibitors: Design,Synthesis, Anti-Proliferative Evaluation,Docking, and MD Simulation Studies

Four new nicotinamide-based derivatives were designed as antiangiogenic VEGFR-2 inhibitors. The congeners were synthesized possessing the pharmacophoric essential features to bind correctly with the VEGFR-2 active pocket. All members were evaluated for their cytotoxic and VEGFR-2 inhibitory potentialities. Compound 6 was the most potent showingIC₅₀ values of 9.3 ± 0.02 and 7.8 ± 0.025 µM against HCT-116 and HepG-2 cells, respectively, and IC₅₀ of 60.83 nM regarding VEGFR-2 enzyme inhibition. Compound 6 arrested the growth of HCT-116 cells at the pre-G1 and G2-M phases. Further, it induced both early and late apoptosis. Additionally, compound 6 caused a significant decrease in TNF-α and IL6 by 66.42% and 57.34%, respectively. The considered compounds had similar docking performances to that of sorafenib against the VEGFR-2 (PDB ID: 2OH4). The correct binding of compound 6 with VEGFR-2 was validated using MD simulations, and MM-GPSA calculations.