Synthesis of 1,2,4-Oxadiazin-5(6)-One Derivatives and Their Biological Investigation as Monoamine Oxidase Inhibitors.

Monoamine oxidase (MAO) plays a key role in the pathogenesis of central nervous system disorders, and MAO inhibitors have been used in the treatment of depression and Parkinson's disease. In the search for new classes of MAO inhibitors, the present study investigated a series of 1,2,4-oxadiazin-5(6)-one derivatives. This study provides the first optimization of the reaction conditions for the condensation of amidoximes with alkyl 2-halocarboxylates to yield the desired 1,2,4-oxadiazin-5(6)-ones.

Effect of nutritional supplements on the physico-structural and sensory characteristics of low-fat camel milk yogurt.

This study aimed to elucidate the effects of various nutritional supplements on the physical, structural and sensory attributes of low-fat yogurt derived from camel milk, with the longer-term objective of enhancing its appeal and suitability for elderly consumers. Fresh camel milk was obtained from an Australian farm. Two yogurt variants were created: plain yogurt (CMY) and yogurt with added fructooligosaccharides, microbial transglutaminase (a ubiquitous food additive with potential health risks), apple pectin and linseed oil (CMYWA).

Extraction of Lignocellulose from Rice Straw and Its Carboxymethylation When Activated by Microwave Radiation.

The paper presents the process of cellulose extraction from rice straw using water-alkaline solution treatment and the subsequent process of carboxymethylation of the obtained product when activated by microwave radiation. After mercerization of rice straw, the obtained product contained 89.2% cellulose and 6.

Progress in the Stereoselective Synthesis Methods of Pyrrolidine-Containing Drugs and Their Precursors.

The presented review systematizes and summarizes the data on the synthesis of pyrrolidine derivatives, which are precursors for obtaining drugs. Based on the analysis of published data, the most promising directions in the synthesis of biologically active compounds containing a pyrrolidine ring are identified. Stereoselective synthesis methods are classified based on the source of the pyrrolidine ring.

Biological Activity Evaluation of Phenolic Isatin-3-Hydrazones Containing a Quaternary Ammonium Center of Various Structures.

A series of new isatin-3-hydrazones bearing different ammonium fragments was synthesized by a simple and easy work-up reaction of Girard's reagents analogs with 1-(3,5-di--butyl-4-hydroxybenzyl)isatin. All derivatives have been shown to have antioxidant properties. In terms of bactericidal activity against gram-positive bacteria, including methicillin-resistant strains of , the best compounds are , , and , bearing octyl, acetal, and brucine ammonium centers, respectively.

Comprehensive overview of heat management methods for enhancing photovoltaic thermal systems.

The paper examines strategies to improve the efficiency of photovoltaic (PV) systems, which are challenged by high operating temperatures that reduce performance. It focuses on enhancing PV systems through the use of gallium arsenide (GaAs) thin films and reviews techniques like spectral beam splitting to boost efficiency, particularly in multi-junction PV receivers and hybrid collectors. The study also explores Photovoltaic-thermal (PVT) systems that combine PV cells with thermal absorbers, highlighting advanced absorber designs, mini/microchannels, and the use of polymers over traditional metals.

Pioneering heat transfer enhancements in latent thermal energy storage: Passive and active strategies unveiled.

Intermittent renewable energy sources such as solar and wind necessitate energy storage methods like employing phase change materials (PCMs) for latent heat thermal energy storage (LHTES). However, the low thermal conductivity of PCMs limits their thermal response rate. This paper reviews recent progress in active heat transfer augmentation methods for improving LHTES system performance, encompassing mechanical aids, vibrations, jet impingement, injection, and external fields.

An efficient RP-HPLC-based approach for simultaneous determination of sitagliptin and metformin HCl in pharmaceutical drug formulation.

This study introduces an innovative, and rapid HPLC method using reverse phase elution for the simultaneous analysis of Sitagliptin and Metformin HCl in pharmaceutical formulations. This combination was explored in bulk and solid dosage forms using Luna Phenomenex C8 column (4.6 x 250 mm, 5 µm) at ambient temperature in isocratic elution.

Impact of Serotonin Transporter Absence on Brain Insulin Receptor Expression, Plasma Metabolome Changes, and ADHD-like Behavior in Mice fed a Western Diet.

The impaired function of the serotonin transporter (SERT) in humans has been linked to a higher risk of obesity and type 2 diabetes, especially as people age. Consuming a "Western diet" (WD), which is high in saturated fats, cholesterol, and sugars, can induce metabolic syndrome. Previous research indicated that mice carrying a targeted inactivation of the gene (knockout, KO) and fed a WD display significant metabolic disturbances and behaviors reminiscent of ADHD.

Insights into the Engineered Gold Nanoparticle-Based Remedy for Supplementation Therapy of Ovarian Carcinoma.

Chronic diseases, notably cancer, pose a significant global threat to human life. Oncologists and medical professionals addressing malignancies confront challenges such as toxicity and multidrug resistance. To tackle these issues, the focus has shifted toward the employment of multifunctional colloidal gold nanoparticles.

Review on Nanofluids: Preparation, Properties, Stability, and Thermal Performance Augmentation in Heat Transfer Applications.

Nanoparticles play a crucial role in enhancing the thermal and rheological properties of nanofluids, making them a valuable option for increasing the efficiency of heat exchangers. This research explores how nanoparticle characteristics, such as concentration, size, and shape, impact the properties of nanofluids. Nanofluids' thermophysical properties and flow characteristics are essential in determining heat transfer efficiency and pressure loss.

Composite Material Based on Polypropylene and Modified Natural Fillers.

The work presents the results of a comprehensive study on obtaining compositions based on polypropylene and natural fillers modified by enzymatic preparations under high-shear forces. The experiment protocol includes determining the modification time and the ratio of water volume to the mass of natural filler (hydro modulus) during modification, which turned out to be different for each type of filler. Physical and mechanical analyses were conducted to evaluate the operational characteristics of the obtained composites, with particular attention given to comparing the modified compositions with their unmodified counterparts.

Conjugates of 3,5-Bis(arylidene)-4-piperidone and Sesquiterpene Lactones Have an Antitumor Effect via Resetting the Metabolic Phenotype of Cancer Cells.

In recent years, researchers have often encountered the significance of the aberrant metabolism of tumor cells in the pathogenesis of malignant neoplasms. This phenomenon, known as the Warburg effect, provides a number of advantages in the survival of neoplastic cells, and its application is considered a potential strategy in the search for antitumor agents. With the aim of developing a promising platform for designing antitumor therapeutics, we synthesized a library of conjugates of 3,5-bis(arylidene)-4-piperidone and sesquiterpene lactones.

Discovery of Di(het)arylmethane and Dibenzoxanthene Derivatives as Potential Anticancer Agents.

A family of bifunctional dihetarylmethanes and dibenzoxanthenes is assembled via a reaction of acetals containing a 2-chloroacetamide moiety with phenols and related oxygen-containing heterocycles. These compounds demonstrated selective antitumor activity associated with the induction of cell apoptosis and inhibition of the process of glycolysis. In particular, bis(heteroaryl)methane containing two 4-hydroxy-6-methyl-2-pyran-2-one moieties combine excellent in vitro antitumor efficacy with an IC of 1.

Superelectrophilic Activation of Phosphacoumarins towards Weak Nucleophiles via Brønsted Acid Assisted Brønsted Acid Catalysis.

The electrophilic activation of various substrates via double or even triple protonation in superacidic media enables reactions with extremely weak nucleophiles. Despite the significant progress in this area, the utility of organophosphorus compounds as superelectrophiles still remains limited. Additionally, the most common superacids require a special care due to their high toxicity, exceptional corrosiveness and moisture sensitivity.

Influence of Partially Carboxylated Powdered Lignocellulose from Oat Straw on Technological and Strength Properties of Water-Swelling Rubber.

The work is aimed at the development of an energy-saving technique involving the partial carboxylation of powdered lignocellulose products from the straw of annual agricultural plants and the use of the obtained products in rubber compositions as a water-swelling filler. Lignocellulose powder from oat straw (composition: α-cellulose-77.0%, lignin-3.

Development of Gluten-Free Bread Production Technology with Enhanced Nutritional Value in the Context of Kazakhstan.

This research aims to enhance the nutritional value of gluten-free bread by incorporating a diverse range of components, including additives with beneficial effects on human health, e.g., dietary fibers.

An Unusual Rearrangement of Pyrazole Nitrene and Coarctate Ring-Opening/Recyclization Cascade: Formal CH-Acetoxylation and Azide/Amine Conversion without External Oxidants and Reductants.

We report an unusual transformation where the transient formation of a nitrene moiety initiates a sequence of steps leading to remote oxidative C-H functionalization (R-CH to R-CHOC(O)R') and the concomitant reduction of the nitrene into an amino group. No external oxidants or reductants are needed for this formal molecular comproportionation. Detected and isolated intermediates and computational analysis suggest that the process occurs with pyrazole ring opening and recyclization.

Anticancer and Antiphytopathogenic Activity of Fluorinated Isatins and Their Water-Soluble Hydrazone Derivatives.

A series of new fluorinated 1-benzylisatins was synthesized in high yields via a simple one-pot procedure in order to explore the possible effect of ortho-fluoro (), chloro (), or bis-fluoro () substitution on the biological activity of this pharmacophore. Furthermore, the new isatins could be converted into water-soluble isatin-3-hydrazones using their acid-catalyzed reaction with Girard's reagent P and its dimethyl analog. The cytotoxic action of these substances is associated with the induction of apoptosis caused by mitochondrial membrane dissipation and stimulated reactive oxygen species production in tumor cells.

Hybrids of Sterically Hindered Phenols and Diaryl Ureas: Synthesis, Switch from Antioxidant Activity to ROS Generation and Induction of Apoptosis.

The utility of sterically hindered phenols (SHPs) in drug design is based on their chameleonic ability to switch from an antioxidant that can protect healthy tissues to highly cytotoxic species that can target tumor cells. This work explores the biological activity of a family of 45 new hybrid molecules that combine SHPs equipped with an activating phosphonate moiety at the benzylic position with additional urea/thiourea fragments. The target compounds were synthesized by reaction of iso(thio)cyanates with C-arylphosphorylated phenols containing pendant 2,6-diaminopyridine and 1,3-diaminobenzene moieties.

Synthesis and Anticancer Evaluation of Novel 7-Aza-Coumarine-3-Carboxamides.

Herein, we report the design and synthesis of novel 7-aza-coumarine-3-carboxamides via scaffold-hopping strategy and evaluation of their in vitro anticancer activity. Additionally, the improved non-catalytic synthesis of 7-azacoumarin-3-carboxylic acid is reported, which features water as the reaction medium and provides a convenient alternative to the known methods. The anticancer activity of the most potent 7-aza-coumarine-3-carboxamides against the HuTu 80 cell line is equal to that of reference Doxorubicin, while the selectivity towards the normal cell line is 9-14 fold higher.

Diverse Biological Activity of Benzofuroxan/Sterically Hindered Phenols Hybrids.

Combining two pharmacophores in a molecule can lead to useful synergistic effects. Herein, we show hybrid systems that combine sterically hindered phenols with dinitrobenzofuroxan fragments exhibit a broad range of biological activities. The modular assembly of such phenol/benzofuroxan hybrids allows variations in the phenol/benzofuroxan ratio.

Bioremediation of Oil-Contaminated Soil of the Republic of Kazakhstan Using a New Biopreparation.

A new biopreparation is developed to clean soils from oil pollution in the arid climate of the Republic of Kazakhstan. The biopreparation includes bacterial strains F2-1, F2-2, and BS3701. When using the biopreparation in a liquid mineral medium with 15% crude oil, laboratory studies have revealed degradation of 48% n-alkanes and 39% of PAHs after 50 days.