The canalicular structure of compact bone in the rat at different ages.

Osteocytes communicate through a canalicular system that maintains the vitality and mineral metabolism of bone. Casting the vascular canals and canaliculi of compact bone with methacrylate and viewing them with scanning electron microscopy shows their extent and relationships. Confocal laser scanning microscopy of the same specimen before corrosion establishes the degree of calcification of the different tissue components. These methods were used to compare basal with alveolar compact bone in the rat mandible at different ages. Sections of the mandibular molar region were placed in a methacrylate resin. After polymerization and study with confocal microscopy, the organic matrix was removed. Juvenile rats had large irregular central vascular canals and lacunae that were more concentric in the basal than the alveolar bone. Cast lacunae were round, and the canaliculi from these lacunae were short and thick in both bones. Adult rats had regular concentrically arranged lacunae in the basal bone. Cast lacunae were ellipsoid and flatter in the basal bone than in the alveolar bone. The intercommunicating canaliculi were increased and canaliculi had more branching than the juvenile rats. The aged rats had fewer vascular canals, lacunae, and canaliculi and had osteoporotic changes. The cast lacunae were slender and flat especially in the basal bone. The porosity of the mandible became more pronounced in the alveolar than in the basal bone with aging. The canaliculi of mandibular compact bone thinned and developed extensive branching with adulthood but decreased in size and number with advanced age. Lacunae proceed from the large circular structures of youth to the flat forms of the aged. These studies show that the internal structure of compact bone changes with age and mirrors its functional state.     

Spectroscopic studies of biologically active organotin(IV) derivatives of 2-[N-(2,4,6-tribromophenylamido]propanoic acid

Herein we describe the synthesis and characterization of compounds having the formulae R₂SnL₂ and R₃SnL, where R = Me, n-Bu, Ph and n-Oct and L = 2-[N-(2,4,6-tribromophenylamido]propanoic acid. All the complexes have been characterized by various spectroscopic methods (IR and ¹H, ¹³C, ¹¹⁹Sn NMR), elemental analysis, mass spectrometry and physical data. These compounds were also screened for their biological activity and found some encouraging results.     

Kinetics of anation of chromium(III) by L-phenylalanine

Summary The kinetics of anation of chromium(III) species, [Cr(H₂O)₆]⁴⁺ and [Cr(H₂O)₅OH]²⁺, by L-phenylalanine in aqueous acid has been studied spectrophotometrically. Effects of varying [substrate], [ligand], [H⁺], , % ethanol and temperature were investigated. The kinetic data suggest a mechanism where outersphere-associations [between chromium(III) species and phenylalanine in the zwitterionic form] precede anation. Comparison of the results with published data suggest an I_a path for the [Cr(H₂O)₆]³⁺ reaction and I_d path for the [Cr(H₂O)₅OH]²⁺ reaction.     

Semiquantitative determination of aromatic andα,β-unsaturated aldehydes by circular thin-layer chromatography

Summary A method for semiquantitative determination of aromatic and,-unsaturated aldehydes such as salicylaldehyde, anisaldehyde, vanillin, veratraldehyde, piperonal, cinnamaldehyde, furfural andp-dimethylaminobenzaldehyde by making circular spots of their isonicotinoyl hydrazones on chromatoplates with circular thin-layer Chromatographic apparatus and their comparison with sensitivity standards has been described. The accuracy is ± 5% and the method is rapid, simple and economical.

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Zusammenfassung Ein Verfahren zur semiquantitativen Bestimmung aromatischer und,-ungesättigter Aldehyde wie Salioylaldehyd, Anisaldehyd, Vanillin, Veratrumaldehyd, Piperonal, Zimtaldehyd, Furfural und p-Dimethylaminobenzaldehyd durch Dünnschicht-Ringchromatographie ihrer Isonikotinsäurehydrazone und Vergleich mit Standardchromatogrammen wurde beschrieben. Die Genauigkeit beträgt ±5%.

     

A new approach for the derivation of bounds for the Jensen difference

There are many useful applications of Jensen's inequality in several fields of science, and due to this reason, a lot of results are devoted to this inequality in the literature. The main theme of this article is to present a new method of finding estimates of the Jensen difference for differentiable functions. By applying definition of convex function, and integral Jensen's inequality for concave function in the identity pertaining the Jensen difference, we derive bounds for the Jensen difference. We present integral version of the bounds in Riemann sense as well. The sharpness of the proposed bounds through examples are discussed, and we conclude that the proposed bounds are better than some existing bounds even with weaker conditions. Also, we present some new variants of the Hermite–Hadamard and Hölder inequalities and some new inequalities for geometric, quasi-arithmetic, and power means. Finally, we give some applications in information theory.     

Circular thin-layer chromatography of aromatic andα,β-unsaturated aldehydes

Summary A simple method based on circular thin-layer chromatography is described for the separation of aromatic and,-unsaturated aldehydes as their isonicotinoyl hydrazones. The development of the chromatoplate is complete within 2 minutes.

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Zusammenfassung Aromatische und,-ungesättigte Aldehyde lassen sich durch ringförmige Dünnschichtchromatographie ihrer Isonikotinoylhydrazone trennen. Die Entwicklung der Dünnschichtplatten ist innerhalb 2 Minuten zu bewerkstelligen.

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Résumé On décrit une méthode simple fondée sur la chromatographie circulaire en couche mince pour séparer les aldéhydes aromatiques et, non saturés, sous forme de leurs hydrazones isonicotinoyles. Le développement de la chromatoplaque est complet en deux minutes.

     

New Triazinoindole Bearing Benzimidazole/Benzoxazole Hybrids Analogs as Potent Inhibitors of Urease: Synthesis,In Vitro Analysis and Molecular Docking Studies

Twenty-four analogs based on triazinoindole bearing benzimidazole/benzoxazole moieties (1–25) were synthesized. Utilizing a variety of spectroscopic methods, including ¹H-, ¹³C-NMR, and HREI-MS, the newly afforded compounds (1–25) were analyzed. The synthesized analogs were tested against urease enzyme (in vitro) as compared to the standard thiourea drug. All triazinoindole-based benzimidazole/benzoxazole analogs (1–25) exhibited moderate to excellent inhibition profiles, having IC₅₀ values of 0.20 ± 0.01 to 36.20 ± 0.70 μM when evaluated under the positive control of thiourea as a standard drug. To better understand the structure–activity relationship, the synthesized compounds were split into two groups, “A” and “B.” Among category “A” analogs, analogs 8 (bearing tri-hydroxy substitutions at the 2,4,6-position of aryl ring C) and 5 (bearing di-hydroxy substitutions at the 3,4-position of aryl ring C) emerged as the most potent inhibitors of urease enzyme and displayed many times more potency than a standard thiourea drug. Besides that, analog 22 (which holds di-hydroxy substitutions at the 2,3-position of the aryl ring) and analog 23 (bearing ortho-fluoro substitution) showed ten-fold-enhanced inhibitory potential compared to standard thiourea among category “B” analogs. Molecular docking studies on the active analogs of each category were performed; the results obtained revealed that the presence of hydroxy and fluoro-substitutions on different positions of aryl ring C play a pivotal role in binding interactions with the active site of the targeted urease enzyme.     

Synthesis,In Vitro Anti-Microbial Analysis and Molecular Docking Study of Aliphatic Hydrazide-Based Benzene Sulphonamide Derivatives as Potent Inhibitors of α-Glucosidase and Urease

A unique series of sulphonamide derivatives was attempted to be synthesized in this study using a new and effective method. All of the synthesized compounds were verified using several spectroscopic methods, including FTIR, ¹H-NMR, ¹³C-NMR, and HREI-MS, and their binding interactions were studied using molecular docking. The enzymes urease and α-glucosidase were evaluated against each derivative (1–15). When compared to their respective standard drug such as acarbose and thiourea, almost all compounds were shown to have excellent activity. Among the screened series, analogs 5 (IC₅₀ = 3.20 ± 0.40 and 2.10 ± 0.10 µM) and 6 (IC₅₀ = 2.50 ± 0.40 and 5.30 ± 0.20 µM), emerged as potent molecules when compared to the standard drugs acarbose (IC₅₀ = 8.24 ± 0.08 µM) and urease (IC₅₀ = 7.80 ± 0.30). Moreover, an anti-microbial study also demonstrated that analogs 5 and 6 were found with minimum inhibitory concentrations (MICs) in the presence of standard drugs streptomycin and terinafine.     

DAD-Net: Classification of Alzheimer’s Disease Using ADASYN Oversampling Technique and Optimized Neural Network

Alzheimer’s Disease (AD) is a neurological brain disorder that causes dementia and neurological dysfunction, affecting memory, behavior, and cognition. Deep Learning (DL), a kind of Artificial Intelligence (AI), has paved the way for new AD detection and automation methods. The DL model’s prediction accuracy depends on the dataset’s size. The DL models lose their accuracy when the dataset has an imbalanced class problem. This study aims to use the deep Convolutional Neural Network (CNN) to develop a reliable and efficient method for identifying Alzheimer’s disease using MRI. In this study, we offer a new CNN architecture for diagnosing Alzheimer’s disease with a modest number of parameters, making it perfect for training a smaller dataset. This proposed model correctly separates the early stages of Alzheimer’s disease and displays class activation patterns on the brain as a heat map. The proposed Detection of Alzheimer’s Disease Network (DAD-Net) is developed from scratch to correctly classify the phases of Alzheimer’s disease while reducing parameters and computation costs. The Kaggle MRI image dataset has a severe problem with class imbalance. Therefore, we used a synthetic oversampling technique to distribute the image throughout the classes and avoid the problem. Precision, recall, F1-score, Area Under the Curve (AUC), and loss are all used to compare the proposed DAD-Net against DEMENET and CNN Model. For accuracy, AUC, F1-score, precision, and recall, the DAD-Net achieved the following values for evaluation metrics: 99.22%, 99.91%, 99.19%, 99.30%, and 99.14%, respectively. The presented DAD-Net outperforms other state-of-the-art models in all evaluation metrics, according to the simulation results.     

Fabrication of PEGylated Chitosan Nanoparticles Containing Tenofovir Alafenamide: Synthesis and Characterization

Tenofovir alafenamide (TAF) is an antiretroviral (ARV) drug that is used for the management and prevention of human immunodeficiency virus (HIV). The clinical availability of ARV delivery systems that provide long-lasting protection against HIV transmission is lacking. There is a dire need to formulate nanocarrier systems that can help in revolutionizing the way to fight against HIV/AIDS. Here, we aimed to synthesize a polymer using chitosan and polyethylene glycol (PEG) by the PEGylation of chitosan at the hydroxyl group. After successful modification and confirmation by FTIR, XRD, and SEM, TAF-loaded PEGylated chitosan nanoparticles were prepared and analyzed for their particle size, zeta potential, morphology, crystallinity, chemical interactions, entrapment efficacy, drug loading, in vitro drug release, and release kinetic modeling. The fabricated nanoparticles were found to be in a nanosized range (219.6 nm), with ~90% entrapment efficacy, ~14% drug loading, and a spherical uniform distribution. The FTIR analysis confirmed the successful synthesis of PEGylated chitosan and nanoparticles. The in vitro analysis showed ~60% of the drug was released from the PEGylated polymeric reservoir system within 48 h at pH 7.4. The drug release kinetics were depicted by the Korsmeyer–Peppas release model with thermodynamically nonspontaneous drug release. Conclusively, PEGylated chitosan has the potential to deliver TAF from a nanocarrier system, and in the future, cytotoxicity and in vivo studies can be performed to further authenticate the synthesized polymer.