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Wyniki wyszukiwania dla: chiral pharmaceuticals
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Metabolic Profiles of New Unsymmetrical Bisacridine Antitumor Agents in Electrochemical and Enzymatic Noncellular Systems and in Tumor Cells
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The Use of Calcium Phosphate-Based Starter Pellets for the Preparation of Sprinkle IR MUPS Formulation of Rosuvastatin Calcium
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On the Absolute Stereochemistry of Tolterodine: A Circular Dichroism Study
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Novel 1,2,4-Oxadiazole Derivatives in Drug Discovery
PublikacjaAbstract: Five-membered 1,2,4-oxadiazole heterocyclic ring has received considerable attention because of its unique bioisosteric properties and an unusually wide spectrum of biological activities. Thus, it is a perfect framework for the novel drug development. After a century since the 1,2,4-oxadiazole have been discovered, the uncommon potential attracted medicinal chemists’ attention, leading to the discovery of a few presently...
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Indole-Acrylonitrile Derivatives as Potential Antitumor and Antimicrobial Agents—Synthesis, In Vitro and In Silico Studies
PublikacjaA series of 2-(1H-indol-2-yl)-3-acrylonitrile derivatives, 2a–x, 3, 4a–b, 5a–d, 6a–b, and 7, were synthesized as potential antitumor and antimicrobial agents. The structures of the prepared compounds were evaluated based on elemental analysis, IR, 1H- and 13NMR, as well as MS spectra. X-ray crystal analysis of the representative 2-(1H-indol-2-yl)-3-acrylonitrile 2l showed that the acrylonitrile double bond was Z-configured. All...
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Phage Therapy—Challenges, Opportunities and Future Prospects
PublikacjaThe increasing drug resistance of bacteria to commonly used antibiotics creates the need to search for and develop alternative forms of treatment. Phage therapy fits this trend perfectly. Phages that selectively infect and kill bacteria are often the only life-saving therapeutic option. Full legalization of this treatment method could help solve the problem of multidrug-resistant infectious diseases on a global scale. The aim of...
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Metabolic Profiles of New Unsymmetrical Bisacridine Antitumor Agents in Electrochemical and Enzymatic Noncellular Systems and in Tumor Cells
PublikacjaNew unsymmetrical bisacridines (UAs) demonstrated high activity not only against a set of tumor cell lines but also against human tumor xenografts in nude mice. Representative UA compounds, named C-2028, C-2045 and C-2053, were characterized in respect to their physicochemical properties and the following studies aimed to elucidate the role of metabolic transformations in UAs action. We demonstrated with phase I and phase II enzymes...
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Bacteriophages as potential tools for use in antimicrobial therapy and vaccine development
PublikacjaThe constantly growing number of people suffering from bacterial, viral, or fungal infections, parasitic diseases, and cancers prompts the search for innovative methods of disease prevention and treatment, especially based on vaccines and targeted therapy. An additional problem is the global threat to humanity resulting from the increasing resistance of bacteria to commonly used antibiotics. Conventional vaccines based on bacteria...
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Regenerative Drug Discovery Using Ear Pinna Punch Wound Model in Mice
PublikacjaThe ear pinna is a complex tissue consisting of the dermis, cartilage, muscles, vessels, and nerves. Ear pinna healing is a model of regeneration in mammals. In some mammals, including rabbits, punch wounds in the ear pinna close spontaneously; in common-use laboratory mice, they remain for life. Agents inducing ear pinna healing are potential regenerative drugs. We tested the effects of selected bioactive agents on 2 mm ear pinna...
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Elucidation of transformation pathway of ketoprofen, ibuprofen, and furosemide in surface water and their occurrence in the aqueous environment using UHPLC-QTOF-MS
PublikacjaThe identification and determination of transformation products (TPs) of pharmaceuticals is essential nowadays, in order to track their fate in the aqueous environment and, thus, to estimate the actual pollution. However, this is a challenging task due to the necessity to apply high-resolution instruments enable to detect known and unknown compounds. This work presents the use of liquid chromatography quadrupole time-of-flight...
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Synthesis and biological activity of mycophenolic acid-amino acid derivatives
PublikacjaIn search of new immunosuppressants, mycophenolic acid (MPA) was coupled with amino acid methyl esters followed by hydrolysis to analogs bearing free carboxylic groups. The obtained compunds were tested in vitro as growth inhibitors of lymphoid cell line (Jurkat) and human peripheral blood mononuclear cells (PBMC) from healthy donors. According to obtained results recovering of free carboxylic group increased their activity. Additionally,...
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Comparative Analysis of Metabolic Variations, Antioxidant Profiles and Antimicrobial Activity of Salvia hispanica (Chia) Seed, Sprout, Leaf, Flower, Root and Herb Extracts
PublikacjaThe purpose of this study was to evaluate the phytochemical profiles of the seeds, sprouts, leaves, flowers, roots and herb of Salvia hispanica and to demonstrate their significant contribution to antioxidant and antimicrobial activities. Applied methods were: HPLC-DAD coupled with post-column derivatization with ABTS reagent, untargeted metabolomics performed by LC-Q-Orbitrap HRMS, and two-fold micro-dilution broth method, which...
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Solubility advantage of sulfanilamide and sulfacetamide in natural deep eutectic systems: experimental and theoretical investigations
PublikacjaObjective: The aim of this study was to explore the possibility of using natural deep eutectic solvents (NADES) as solvation media for enhancement of solubility of sulfonamides, as well as gaining some thermodynamic characteristics of the analyzed systems. Significance: Low solubility of many active pharmaceutical ingredients is a well-recognized difficulty in pharmaceutical industry, hence the need for different strategies addressing...
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Potential Skyrmion Host Fe(IO3)3: Connecting Stereoactive Lone-Pair Electron Effects to the Dzyaloshinskii-Moriya Interaction
PublikacjaMagnetic skyrmions, which are topologically distinct magnetic spin textures, are gaining increased attention for their unique physical properties and potential applications in spintronic devices. Here we present a design strategy for skyrmion host candidates based on combinations of magnetic spin, asymmetric building units having stereoactive lone-pair electrons, and polar lattice symmetry. To demonstrate the viability of the proposed...
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Solubility Characteristics of Acetaminophen and Phenacetin in Binary Mixtures of Aqueous Organic Solvents: Experimental and Deep Machine Learning Screening of Green Dissolution Media
PublikacjaThe solubility of active pharmaceutical ingredients is a mandatory physicochemical characteristic in pharmaceutical practice. However, the number of potential solvents and their mixtures prevents direct measurements of all possible combinations for finding environmentally friendly, operational and cost-effective solubilizers. That is why support from theoretical screening seems to be valuable. Here, a collection of acetaminophen...
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Problematyka dotycząca zapewnienia fotostabilności substancji leczniczych w postaciach leku
PublikacjaUV and visible radiation may influence on the stability of some active pharmaceutical ingredients and in a consequence destabilizes such medicinal products, causes changesin its physicochemical properties also with negative pharmacological and sometimes even toxic effects. For this reason it is important to conduct the routine testing photostability. The knowledge of chemistry and technology as well as some methods of...
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Determination of API content in a pilot-scale blending by near-infrared spectroscopy as a first step method to process line implementation
PublikacjaNear infrared (NIR) spectroscopy was used for estimation of powder blend homogeneity and manufacturing control of a medicinal product powder mixture containing active pharmaceutical ingredient (API). Aiming at initiating a Process Analytical Technology (PAT) activity, the first step was a stationary mode atline evaluation. In this, the content of pharmaceutical active compound in the powder mixtures intended to the direct tabletting...
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Structure elucidation of carbamoylo-β-lactam diastereoisomers by ROESY and NOESY experiments
PublikacjaRecently we have focused in the problem of preparation of carbamoylo-β-lactams as a result of oxidative cyclization of malonyl enamides. In our experiments we obtain mixture of two main β-lactam products: as a result of subsequent elimination and a second as a product of substitution. All of the produced β-lactams have trans configuration what was confirmed by 1H coupling constants. However id should be stressed that in the case...
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The role of the One-Belt One-Road initiative in China's exports and global value chains
PublikacjaResearch background: China is regarded as the “world factory” highly involved in international trade and plays an increasingly important role in the global value chains (GVC). Additionally, the “One-Belt One-Road” (OBOR) initiative was proposed by the Chinese government to further promote China in the international market. Purpose of the article: The article explores the role of the OBOR in China’s exports and global value...
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The complete stereochemistry of the antibiotic candicidin A3 (syn. ascosin A3, levorin A3)
PublikacjaHerein, the stereostructure of the aromatic heptaene macrolide (AHM) antifungal antibiotic candicidin A3 (syn. ascosin A3, levorin A3) has been established upon the 2D NMR studies, consisting of DQF-COSY, TOCSY, ROESY, HSQC and HMBC experiments, as well as upon extensive molecular dynamics simulations. The geometry of the heptaenic chromophore was defined as: (22E, 24E, 26Z, 28Z, 30E, 32E, 34E). The previously unreported absolute...
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Self-Association of Amphotericin B: Spontaneous Formation of Molecular Structures Responsible for the Toxic Side Effects of the Antibiotic
PublikacjaAmphotericin B (AmB) is a lifesaving antibiotic used to treat deep-seated mycotic infections. Both the pharmaceutical activity and highly toxic side effects of the drug rely on its interaction with biomembranes, which is governed by the molecular organization of AmB. In the present work we present detailed analysis of self-assembly of AmB molecules in different environments, interesting from the physiological standpoint, based...
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Evidence of mutations conferring resistance to clarithromycin in wastewater and activated sludge
PublikacjaThe occurrence of clarithromycin in wastewater samples and of the activated sludge bacteria possibly resistant to this pharmaceutical was the object of the study. Samples of wastewater or activated sludge were taken from a municipal wastewater treatment plant in summer and winter and characterised regarding their clarithromycin concentrations and the presence of nucleic acid fragments (Cla-sequences) known to be responsible for...
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In Vitro Biological Evaluation of Aprepitant Based 177Lu-Radioconjugates
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The Stimulating Effect of Rosmarinic Acid and Extracts from Rosemary and Lemon Balm on Collagen Type I Biosynthesis in Osteogenesis Imperfecta Type I Skin Fibroblasts
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The Correlation between Physical Crosslinking and Water-Soluble Drug Release from Chitosan-Based Microparticles
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Hydrogel Delivery System Containing Calendulae flos Lyophilized Extract with Chitosan as a Supporting Strategy for Wound Healing Applications
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The Chitosan-Based System with Scutellariae baicalensis radix Extract for the Local Treatment of Vaginal Infections
PublikacjaScutellarie baicalensis radix, as a flavone-rich source, exhibits antibacterial, antifungal, an-tioxidant, and anti-inflammatory activity. It may be used as a therapeutic agent to treat various
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Recent Advances in Polymer-Based Vaginal Drug Delivery Systems
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Photoprotection and Antiaging Activity of Extracts from Honeybush (Cyclopia sp.)—In Vitro Wound Healing and Inhibition of the Skin Extracellular Matrix Enzymes: Tyrosinase, Collagenase, Elastase and Hyaluronidase
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Nanoemulsion Structural Design in Co-Encapsulation of Hybrid Multifunctional Agents: Influence of the Smart PLGA Polymers on the Nanosystem-Enhanced Delivery and Electro-Photodynamic Treatment
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Effective Targeting of Colon Cancer Cells with Piperine Natural Anticancer Prodrug Using Functionalized Clusters of Hydroxyapatite Nanoparticles
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Abdominoplasty Skin-Based Dressing for Deep Wound Treatment—Evaluation of Different Methods of Preparation on Therapeutic Potential
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Tuning of the Anti-Breast Cancer Activity of Betulinic Acid via Its Conversion to Ionic Liquids
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New Peptide Based Fluconazole Conjugates with Expanded Molecular Targets
PublikacjaInfections of Candida spp. etiology are frequently treated with azole drugs. Among azoles, the most widely used in the clinical scenario remains fluconazole (FLC). Promising results in treatment of dangerous, systemic Candida infections demonstrate the advantages of combined therapies carried out with combinations of at least two different antifungal agents. Here, we report five conjugates composed of covalently linked FLC and...
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pH-Responsive Drug Delivery Nanoplatforms as Smart Carriers of Unsymmetrical Bisacridines for Targeted Cancer Therapy
PublikacjaSelective therapy and controlled drug release at an intracellular level remain key challenges for effective cancer treatment. Here, we employed folic acid (FA) as a self-navigating molecule in nanoconjugates containing quantum dots (QDs) and β-cyclodextrin (β-CD) for the delivery of antitumor unsymmetrical bisacridine compound (C-2028) to lung and prostate cancers as well as normal cells. The bisacridine derivative can form the...
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Synergistic Effects of Propolis Combined with 2-Phenoxyethanol and Antipyretics on the Growth of Staphylococcus aureus
PublikacjaThe present investigation aimed to assess the combinational effect of commonly usedantipyretics and antiseptics with ethanolic extracts of propolis (EEPs) on the growth inhibition ofStaphylococcus aureus. The broth microdilution checkerboard assay revealed synergistic interactionsbetween all investigated antipyretics, namely acetylsalicylic acid, ibuprofen, and acetaminophen,with EEPs samples. The values of the fractional inhibitory...
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Spectroscopic evaluation on pseudopolymorphs of sodium naproxen
PublikacjaThis paper demonstrates the assessment of vibrational spectroscopy methods such as middle infrared, near infrared and Raman spectroscopy (FTIR, FT-NIR, Raman) for the identification of pseudopolymorphic forms of a model active pharmaceutical ingredient (API) - sodium naproxen (NpxNa). NpxNa, in the form of three different pseudopolymorphs, was investigated by methods dedicated for solid state characterization: DSC (differential...
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Biopolymers and Their Composites for Drug Delivery: A Brief Review
PublikacjaIn recent years, excipient development has become a core area of research in pharmaceutical drug delivery because it influences the formulation development and drug delivery process in various ways. Polymeric drug delivery systems have been of great interest for controlled delivery as they show the great advantage in drug delivery systems because of optimized drug loading and releasing property. Then, the side effects of synthetic...
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Polysaccharide nanocomposites in wastewater treatment: A review
PublikacjaIn modern times, wastewater treatment is vital due to increased water contamination arising from pollutants such as nutrients, pathogens, heavy metals, and pharmaceutical residues. Polysaccharides (PSAs) are natural, renewable, and non-toxic biopolymers used in wastewater treatment in the field of gas separation, liquid filtration, adsorption processes, pervaporation, and proton exchange membranes. Since addition of nanoparticles...
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Characteristic and specificity of protease activity of thermophilic bacteria Meiothermus ruber
PublikacjaThe primary purpose of research was to establish the possibility of using thermophilic bacteria Meiothermus ruber as a source of proteolytic enzymes. The main reason of searching new proteases is their commercial value especially in production of detergents, food, pharmaceuticals, leather, diagnostics or waste management. The development of this type processes will be possible by utilization of enzymes which have unique characteristics...
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Spin and Orbital Effects on Asymmetric Exchange Interaction in Polar Magnets: M(IO3)2 (M = Cu and Mn)
PublikacjaMagnetic polar materials feature an astonishing range of physical properties, such as magnetoelectric coupling, chiral spin textures, and related new spin topology physics. This is primarily attributable to their lack of space inversion symmetry in conjunction with unpaired electrons, potentially facilitating an asymmetric Dzyaloshinskii–Moriya (DM) exchange interaction supported by spin–orbital and electron–lattice coupling. However,...
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China’s international trade and global value chains under One-Belt One-Road initiative
PublikacjaResearch background: After China acceded to the WTO in 2001, its foreign trade has expanded rapidly to be the largest share in the world. However, China's economic development changing from high-speed growth to medium high-speed growth in recent years. At the same time, the increase in labour cost and overcapacity also hinder China’s international trade. In order to solve these challenges and strengthening ties...
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Abuse or contamination? Ratio determination of clenbuterol enantiomers to distinguish between doping use and meat contamination
PublikacjaClenbuterol has been detected in urine of several athletes during routine doping control in the past years. Athletes claimed that the clenbuterol was ingested by eating contaminated meat. Providing analytical prove for this claim is difficult. clenbuterol consists of two enantiomers, R(-) and S(+)-clenbuterol. Currently available human and veterinary preparations were found to consist of a racemic mixture of both enantiomers. When...
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The impact of China’s One-Belt One-Road initiative on international trade and global value chains
PublikacjaThis study examines the potential effects of China’s ‘One-Belt One-Road’initiative (OBOR) on trade flows and global value chain (GVC) connections.The empirical analysis is based on the augmented trade gravity model, which comprises 186 economies and 199 of their partners from 2000 to 2018. We also estimate the gravity model for involvement in GVC (domestic value added in intermediate exports, foreign value added in exports, and...
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Nanoparticles: Taking a Unique Position in Medicine
PublikacjaThe human nature of curiosity, wonder, and ingenuity date back to the age of humankind. In parallel with our history of civilization, interest in scientific approaches to unravel mechanisms underlying natural phenomena has been developing. Recent years have witnessed unprecedented growth in research in the area of pharmaceuticals and medicine. The optimism that nanotechnology (NT) applied to medicine and drugs is taking serious...
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THERMAL ANALYSIS AND DESIGN OF HYBRID MICROCHANNEL -MICROJET TEST PROBE
PublikacjaAccurate control of cooling parameters is required in ever wider range of technical applications. It is known that reducing the flow hydraulic diameter to an increase in the economy of cooling and improves its quality (Mikielewicz and Muszyński 2009). Present study describes research results related to the design and construction of the test stand for hybrid microjet- microchannel cooling modules study, which may be applied in...
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Natural Deep Eutectic Solvents as Agents for Improving Solubility, Stability and Delivery of Curcumin
PublikacjaPurpose Study on curcumin dissolved in natural deep eutectic solvents (NADES) was aimed at exploiting their beneficial properties as drug carriers. Methods The concentration of dissolved curcumin in NADES was measured. Simulated gastrointestinal fluids were used to determine the concentration of curcumin and quantum chemistry computations were performed for clarifying the origin of curcumin solubility enhancement in NADES. Results NADES...
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Biological activities of leaf extracts from selected Kalanchoe species and their relationship with bufadienolides content
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Biodegradable Poly(ester-urethane) Carriers Exhibiting Controlled Release of Epirubicin
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Magnetically recyclable TiO2/MXene/MnFe2O4 photocatalyst for enhanced peroxymonosulphate-assisted photocatalytic degradation of carbamazepine and ibuprofen under simulated solar light
PublikacjaIn this study, a novel TiO2/Ti3C2/MnFe2O4 magnetic photocatalyst with dual properties, enabling (i) improved photocatalytic degradation with PMS activation under simulated solar light and (ii) magnetic separation after the degradation process in an external magnetic field was developed and applied for the efficient photodegradation pharmaceutically active compounds (PhACs) frequently present in wastewater and surface waters worldwide. MXene...