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Search results for: FLAVONOID DERIVATIVES
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2,6-Bis((benzoyl-R)amino)pyridine (R = H, 4-Me, and 4-NMe2) Derivatives for the Removal of Cu(II), Ni(II), Co(II), and Zn(II) Ions from Aqueous Solutions in Classic Solvent Extraction and a Membrane Extraction
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Influence of different cultivation systems on bioactivity of asparagus
PublicationEvaluation of functional and bioactive compounds of Asparagus officinalis L. growing in conventional and organic greenhouse and conventional open –field farming was the aim of this research. Polyphenols in cladodes grown conventionally were higher than organic. Flavonoids and carotenoids were the highest in cladodes in open field. Organic spears were richer in total phenolics (+6.9% and +19.1%) and flavonoids (+4.7% and 16.8%)...
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Electron-Induced Decomposition of 5-Bromo-4-thiouracil and 5-Bromo-4-thio-2′-deoxyuridine: The Effect of the Deoxyribose Moiety on Dissociative Electron Attachment
PublicationWhen modified uridine derivatives are incorporated into DNA, radical species may form that cause DNA damage. This category of molecules has been proposed as radiosensitizers and is currently being researched. Here, we study electron attachment to 5-bromo-4-thiouracil (BrSU), a uracil derivative, and 5-bromo-4-thio-20 -deoxyuridine (BrSdU), with an attached deoxyribose moiety via the N-glycosidic (N1-C) bond. Quadrupole mass spectrometry...
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Biologically active compounds based on the carbazole scaffold - synthetic and mechanistic aspects
PublicationDoctoral dissertation is divided into three main parts: introduction, results and discussion and experimental. The introduction is divided into four main parts which describe: 5-hydroxytryptamine receptors, the most popular antidepressants, new compounds based on the carbazole structure with affinity for serotonin receptors, telomeres and telomerase with their functions, telomerase inhibition strategies, carbazoles approved in...
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Detection of Bioactive Compounds in Organically and Conventionally Grown Asparagus Spears
PublicationIn the recent reports, there are contradictory conclusions about the nutritional and health properties of organic and conventionally growing vegetables. We hypothesized that organic cultivation system results in higher quality of asparagus (Asparagus officinalis L.) because of organic manure and effective organisms. Therefore, new analytical methods were applied in order to find the differences in bioactive compounds between the...
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Development and evaluation of thermosensitive hydrogels with binary mixture of Scutellariae baicalensis radix extract and chitosan for periodontal diseases treatment.
PublicationScutellaria baicalensis root displays anti-inflammatory and antibacterial properties due to the presence of flavonoids, particularly baicalin, baicalein, and wogonin. Our work aimed at developing thermosensitive hydrogels containing a binary mixture of S. baicalensis radix lyophilized extract and chitosan as a novel approach for periodontal diseases treatment....
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Zero-pole approach to computer aided design of in-line siw filters with transmission zeros
PublicationThis paper presents a design of a new type of in-line pseudo-elliptic filters implemented in substrate integrated waveguide(SIW) technology. To realize transmission zeros in in-line topology,frequency-dependent couplings were used. Such dispersive couplingswere implemented as shorted stubs. The design process startswith the generation of a suitable starting point. To this end, anapproximation of SIW as a rectangular waveguide is...
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Novel 2-(2-arylmethylthio-4-chloro-5-methylbenzenesulfonyl)-1-(1,3,5-triazin-2-ylamino)guanidine derivatives: Inhibition of human carbonic anhydrase cytosolic isozymes I and II and the transmembrane tumor-associated isozymes IX and XII, anticancer activity, and molecular modeling studies
PublicationA series of novel 2-(2-arylmethylthio-4-chloro-5-methylbenzenesulfonyl)-1-(6-substituted-4-chloro-1,3,5-triazin-2-ylamino)guanidine derivatives 9–20 have been synthesized by substitution of chlorine atom at the 1,3,5-triazine ring in compounds 5–8 with 3- or 4-aminobenzenesulfonamide and 4-(aminomethyl)benzenesulfonamide hydrochloride. All the synthesized compounds were evaluated for their inhibitory activity toward hCA I, II,...
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Preparation of Pseudopeptides Building Blocks with Retro-Thioamide Bond Mediated via Thiocarbamoyl Meldrum's Acid
PublicationAn easy and efficient synthesis of pseudo tripeptide containing a thiomalonamide moiety was developed. Isothiocyanate derivatives of amino acids react smoothly with 2,2-dimethyl-1,3-dioxane-4,6-dione yielding new thiocarbamoyl Meldrum's acids. Thermal decomposition of this new Meldrum's acid derivatives generate thiocarbamoyl ketenes, which acylate amino acid esters to give pseudo tripeptides.
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The Substantial Improvement of Amphotericin B Selective Toxicity Upon Modification of Mycosamine with Bulky Substituents
PublicationAbstract: Background: It is assumed that the unfavorable selective toxicity of an antifungal drug Amphotericin B (AmB) can be improved upon chemical modification of the antibiotic molecule. Objective: The aim of this study was verification of the hypothesis that introduction of bulky substituents at the amino sugar moiety of the antibiotic may result in diminishment of mammalian vitro toxicity of thus prepared AmB derivatives. Methods:...
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Synthesis, molecular structure, and metabolic stability of new series of N' -(2-alkylthio-4-chloro-5-methylbenzenesulfonyl)-1-(5-phenyl-1 H -pyrazol-1-yl)amidine as potential anti-cancer agents
PublicationA series of new N'-(2-alkylthio-4-chloro-5-methylbenzenesulfonyl)-1-(5-phenyl-1H-pyrazol-1-yl)amidine derivatives have been synthesized and evaluated in vitro by MTT assays for their antiproliferative activity against cell lines of colon cancer HCT-116, cervical cancer HeLa and breast cancer MCF-7. The studied compounds display selective activity mainly against HCT-116 and HeLa cells. Thus, five compounds show selective cytotoxic...
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New bis(azobenzocrown)s with dodecylmethylmalonyl linkers as ionophores for sodium selective potentiometric sensors
PublicationNovel biscrowns 1 and 2 were synthesized from 13-membered azobenzocrown ethers containing bromoalkylenoxy chains in para position relative to the azo group. The synthesized diester molecules are dodecylmethylmalonic acid derivatives differing by the linker length. The synthesized compounds have the potential of being used as sodium ionophores in ion-selective electrodes. They were characterized and used as ionophores in classic...
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The thermostability, bioactive compounds and antioxidant activity of some vegetables subjected to different durations of boiling: investigation in vitro
PublicationThis research was performed in order to compare the water and acetone extracts of raw and boiled for 10, 20, 40 and 60 min Korean lotus roots (KLR) and Polish white onion (PWO) in the contents of theirbioactive compounds, antioxidant activity and thermostability.It was found that polyphenols (mg GAE/g), flavanols (mg GAE/g), flavonoids (mg CE/g), anthocyanins (mg CGE/kg) and tannins (mg CE/g) in water extract of raw lotus roots...
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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
PublicationThe 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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Cuticular lipids of insects as potential biofungicides
PublicationThe term ''lipids'' refers to fatty acids, their derivatives and substances related with them biochemically or by the functions in the body. Lipids include compounds with different chemical structure. There are lipids with structures based on long-chain carboxylic acids and their direct derivatives, namely: fatty acids, alkanes, some alkenes, aldehydes and long chain alcohols and their derivatives (esters). The variety of lipid...
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In vitro evaluation of novel lipopeptides with potential therapeutic application
PublicationThe synthesis of derivatives of Gly-His-Lys was elaborated followed by their antimicrobial activity investigation.
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Cooperativity of Halogen- and Chalcogen-Bonding Interactions in the Self-Assembly of 4‑Iodoethynyl- and 4,7-Bis(iodoethynyl)benzo-2,1,3-chalcogenadiazoles: Crystal Structures, Hirshfeld Surface Analyses, and Crystal Lattice Energy Calculations
PublicationSeveral new 4-iodoethynyl- and 4,7-bis- (iodoethynyl)benzo-2,1,3-chalcogenadiazoles were prepared, and a comprehensive analysis of the most prominent secondary bonding interactions responsible for the crystal self-assembly was performed using X-ray diffraction. The presence of both the iodoethynyl and chalcogenadiazole moieties allows an evaluation of the preference of these molecules to aggregate through either chalcogen- or halogen-bonding...
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Starch–metal complexes and metal compounds
PublicationRecently, metal derivatives of starch evoked considerable interest. Such metal derivatives can take a form of starch compounds bearing metal atoms and metal carrying moieties either covalently bound or complexed. Starch metal complexes may have a character of either Werner, inclusion, sorption or capillary complexes. In this publication, preparation, structure, properties and numerous current and potential applications of those...
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Graphene Reinforced Phenolic Foams
PublicationPhenolic foams (PF) belong to the polymeric materials, which are very attractive from the point of many possible applications such as insulation or fire protection materials. This chapter attempts to explain the influence of graphene and graphene derivatives on the phenolic foams. This work briefly presents different graphene nanoparticles introduced to the phenolic foams matrix, in terms of impact on the thermal, mechanical, and...
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Analysis of latency between quotations and capital flow in capital markets.
PublicationThe aim of this paper is to prove that the derivative of the log of capital flow understood as price times volume advances the derivative of log of the price. A certain concept of signal processing using linear filtering has been proposed to conduct the research.
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The termostability, bioactive compounds and antioxidant activity of some vegetables subjected to different durations of boiling: investigation in vitro.
PublicationThis research was performed in order to compare the water and acetone extracts of raw and boiled for 10, 20, 40 and 60 min Korean lotus roots (KLR) and Polish white onion (PWO) in the contents of theirbioactive compounds, antioxidant activity and thermostability. It was found that polyphenols (mg GAE/g), flavanols (mg GAE/g), flavonoids (mg CE/g), anthocyanins(mg CGE/kg) and tannins (mg CE/g) in water extract of raw lotus roots...
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Efficient Synthesis of Functionalized Unsymmetrical Dialkyl Trisulfanes
PublicationWe have developed a convenient method for the synthesis of functionalized unsymmetrical dialkyl trisulfanes under mild conditions in very good yields. The designed method is based on the reaction of (5,5-dimethyl-2-thioxo-1,3,2-dioxaphosphorinan-2-yl)-disulfanyl derivatives with alkyl disulfanyl anions generated in situ from S-acetyl disulfanyl derivatives and sodium methoxide. The developed method allows for the preparation of...
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Highly effective degradation of selected groups of organic compounds by cavitation based AOPs under basic pH conditions
PublicationCavitation has become on the most often applied methods in a number of industrial technologies. In the case of oxidation of organic pollutants occurring in the aqueous medium, cavitation forms the basis of numerous advanced oxidation processes (AOPs). This paper presents the results of investigations on the efficiency of oxidation of the following groups of organic compounds: organosulfur, nitro derivatives of benzene, BTEX, and...
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9,10-Dioxoanthracenyldithiocarbamates effectively inhibit the proliferation of non-small cell lung cancer by targeting multiple protein tyrosine kinases
PublicationAnthraquinones have attracted considerable interest in the realm of cancer treatment owing to their potent anticancer properties. This study evaluates the potential of a series of new anthraquinone derivatives as anticancer agents for non-small-cell lung cancer (NSCLC). The compounds were subjected to a range of tests to assess their cytotoxic and apoptotic properties, ability to inhibit colony formation, pro-DNA damage functions,...
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Novel and Efficient Methods for the Synthesis of Symmetrical Trisulfides
PublicationWe have developed a convenient methods for the synthesis of symmetrical trisulfides under mild conditions in very good yields. The described methods are based on the straightforward preparation of 5,5-dimethyl-2-thioxo-1,3,2-dioxaphosphorinane-2-disulfanyl derivatives from readily available 5,5-dimethyl-2-sulfanyl-2-thioxo-1,3,2-dioxaphosphorinane or bis(5,5-dimethyl-2-thioxo-1,3,2-dioxaphosphorinan-2-yl) disulfide. The symmetrical...
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The smoothness test for a density function
PublicationThe problem of testing hypothesis that a density function has no more than μ derivatives versus it has more than μ derivatives is considered. For a solution, the L2 norms of wavelet orthogonal projections on some orthogonal ‘‘differences’’ of spaces from a multiresolution analysis is used. For the construction of the smoothness test an asymptotic distribution of a smoothness estimator is used. To analyze that asymptotic distribution,...
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TBAF Promoted Formation of Symmetrical Trisulfides
PublicationWe have developed a new method for the synthesis of functionalized symmetrical trisulfides based on (5,5-dimethyl-2-thioxo-1,3,2-dioxaphosphorin-2-yl)disulfanyl derivatives prepared from readily available 5,5-dimethyl-2-sul-fanyl-2-thioxo-1,3,2-dioxaphosphorinane or bis(5,5-dimethyl-2-thioxo-1,3,2-dioxaphosphorinan-2-yl) disulfide. The symmetrical trisulfides can be obtained from aliphatic and aromatic thiols andL-cysteine derivatives...
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Opracowanie dogodnej metody tworzenia wiązań S-C o hybrydyzacji atomu węgla sp oraz sp2
PublicationBadania przeprowadzone w Katedrze Chemii Organicznej Wydziału Chemicznego Politechniki Gdańskiej na przestrzeni ostatnich kilku lat, pokazały wszechstronność pochodnych kwasu neopentylidenofosforoditiowego. Dotychczasowe wyniki badań doprowadziły mnie do opracowania nowych strategii syntetycznych, umożliwiających otrzymywanie związków zawierających wiązanie C-S o hybrydyzacji atomu węgla sp oraz sp2. Analizując wyniki badań opracowałam...
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Selection of derivatisation agents for chlorophenols determination with multicriteria decision analysis
PublicationThe paper shows very systematic method of selection of derivatisation agents for a given group of analytes. In this study 8 derivatisation agents are assessed for their capability to derivatise 8 chlorophenols. Multicriteria decision analysis is used to combine many objectives of derivatisation agents selection into single, easy to be interpreted numerical value. Three basic analyses were performed to obtain rankings with the aims...
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Comparative assessment of two extraction procedures for determination of bioactive compounds in some berries used for daily food consumption
PublicationTwo extractions with methanol and water were used to determine the antioxidant and binding properties of some berries as a supplement to food. Fluorometry, FTIR spectra and radical scavenging assays were used for characterisation of bioactive compounds (polyphenols, flavonoids, flavanols and tannins) and the levels of their antioxidant activities (AAs). The contents of bioactive compounds and AAs in water and methanol polyphenol...
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Sensorless algorithm for sustaining controllability of IPMSM drive in electric vehicle after resolver fault
PublicationThis paper presents a sensorless algorithm designated for the emergency control of an interior permanent magnet synchronous motor (IPMSM) drive in electric or hybrid vehicle. The algorithm is based on analysing the derivatives of motor phase currents measured over the duration of particular inverter states. The method is computationally simple and does not require additional hardware since the derivatives are measured indirectly....
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Synthesis and steroid sulfatase inhibitory activities of N-phosphorylated 3-(4-aminophenyl)-coumarin-7-O-sulfamates
PublicationIn the present work, we report convenient methods for the synthesis and biological evaluation of N-phosphorylated derivatives of 3-(4-aminophenyl)-coumarin-7-O-sulfamate as potential steroid sulfatase (STS) inhibitors. Their binding modes were modeled using docking techniques. The inhibitory effects of the synthesized compounds were tested on STS isolated from human placenta. All of the newly synthesised coumarin derivatives were...
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Naturalne związki organiczne
PublicationKsiążka zawiera dwanaście rozdziałów merytorycznych, w których omówiono występowanie, właściwości, otrzymywanie i zastosowanie następujących naturalnych organicznych: aminokwasy, peptydy, białka, cukry, lipidy, alkaloidy, steroidy, kwasy nukleinowe, polifenole i flawonoidy, hormony owadzie i roślinne, terpenoidy i izoterpenoidy oraz związki sygnałowe (feromony).
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Sum-over-state expressions including second-order Herzberg–Teller effects for the calculation of absorption and resonance Raman intensities
PublicationThe sum-over-state expressions are derived to calculate the second-order Herzberg–Teller (HT) effects in absorption and resonance Raman spectroscopies. These effects depend on the second derivatives of the transition dipole moment with respect to the vibrational coordinates. The method is applied to the molecule of 1,3-butadiene using density functional theory calculations. It is found that the second-order HT effects are significant...
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Modifications at the C(5) position of pyrimidine nucleosides
PublicationThis review summarizes the state of knowledge on the chemical methods of C(5)-modifications of uridine and cytidine derivatives and may serve as a useful tool for synthetic chemists to choose an appropriate reaction protocol. The synthesis of 5-substituted uracil derivatives is gaining an increasing interest because of their possible applications in medicine and pharmacy. Modifications at the C(5) position of pyrimidine nucleosides...
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Approaches Towards Better Immunosuppressive Agents
PublicationSeveral classes of compounds are applied in clinics due to their immunosuppressive properties in transplantology and the treatment of autoimmune diseases. Derivatives of mycophe-nolic acid, corticosteroids and chemotherapeutics bearing heterocyclic moieties like methotrexate, azathioprine, mizoribine, and ruxolitinib are active substances with investigated mechanisms of action. However, improved synthetic approaches of known drugs...
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Recent developmentsinthesynthesisand biological activityofacridine/acridoneanalogues
PublicationMany people in the world struggle with cancer or bacterial, parasitic, viral, Alzheimer's and other diseases. Therefore, many scientists seek new, more effective, more selective and less toxic drugs. Acridine/acridone derivatives constitute a class of compounds with a broad spectrum of biological activity and are of great interest to scientists. Todate, many acridine/acridone analogues have been obtained,which, inter alia, exhibit...
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A new and convenient method for the preparation of functionalized phosphorothioates
PublicationA new and efficient method for the synthesis of alkyl and aryl phosphorothioates in high yields via the reaction of (5,5-dimethyl-2-thioxo-1,3,2-dioxaphosphorin-2-yl)disulfanyl derivatives with trimethyl phosphite was developed.
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From tryptophan to novel mitochondria-disruptive agent, synthesis and biological evaluation of 1,2,3,6-tetrasubstituted carbazoles
PublicationMitochondrial targeting plays an important role in anticancer therapy. The Mn(III)-promoted cyclization of 5- (1H-indol-3-yl)-3-oxopentanoic acid allow to obtain novel substituted carbazole derivatives that can act as mitochondria-disruptive agents. The starting materials used for the synthesis of these new aminocarbazoles are oxopentanoate derivatives of tryptophan. The scope and limitation of this method of synthesis are determined...
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Numerical Investigation of Nuclear Reactor Kinetic and Heat Transfer Fractional Model with Temperature Feedback
PublicationAbstract—In the paper, the numerical results concerning the kinetics and proposed heat exchange models in nuclear reactor based on fractional calculus are presented for typical inputs. Two fractional models are proposed and compared with the model based on ordinary derivative. The first fractional model is based on one of the generalized Cattaneo equations. The second one is based on replacing the ordinary to fractional order of...
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Influence of Diosmin Treatment on the Level of Oxidative Stress Markers in Patients with Chronic Venous Insufficiency
PublicationOxidative stress plays an important role in the pathophysiology of many human disorders, while antioxidants prevent the development of various adverse symptoms. Diosmin is a natural flavonoid applied in vascular system disorders, especially in chronic venous insufficiency (CVI), and it plays a significant part in the alleviation of CVI symptoms. Due to antioxidant activity, it also has the ability to scavenge the oxygen free radicals...
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Synthesis and Spectroscopic Characterization of Selected Phenothiazines and Phenazines Rationalized Based on DFT Calculation
PublicationTwo unique structures were isolated from the phosphorylation reaction of 10H-phenothiazine.The 5,5-dimethyl-2-(10H-phenothiazin-10-yl)-1,3,2-dioxaphosphinane 2-oxide (2a) illustrates theproduct of N-phosphorylation of phenothiazine. Moreover, a potential product of 2a instability,a thiophosphoric acid 2b, was successfully isolated and structurally characterized. Molecule 2a,similarly to sulfoxide derivative...
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Synthesis of Cyano-Benzylidene Xanthene Synthons Using a Diprotic Brønsted Acid Catalyst, and Their Application as Efficient Inhibitors of Aluminum Corrosion in Alkaline Solutions
PublicationNovel cyano-benzylidene xanthene derivatives were synthesized using one-pot and condensation reactions. A diprotic Brønsted acid (i.e., oxalic acid) was used as an effective catalyst for the promotion of the synthesis process of the new starting xanthene–aldehyde compound. Different xanthene concentrations (ca. 0.1–2.0 mM) were applied as corrosion inhibitors to control the alkaline uniform corrosion of aluminum. Measurements were...
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Discrete and continuous fractional persistence problems – the positivity property and applications
PublicationIn this article, we study the continuous and discrete fractional persistence problem which looks for the persistence of properties of a given classical (α=1) differential equation in the fractional case (here using fractional Caputo’s derivatives) and the numerical scheme which are associated (here with discrete Grünwald–Letnikov derivatives). Our main concerns are positivity, order preserving ,equilibrium points and stability...
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Structural factors affecting affinity of cytotoxic oxathiole-fused chalcones toward tubulin
PublicationSynthesis, in vitro cytotoxic activity, and interaction with tubulin of (E)-1-(6-alkoxybenzo[d][1,3]oxathiol- 5-yl)-3-phenylprop-2-en-1-one derivatives (2) are described. Some of the compounds demonstrated cytotoxic activity at submicromolar concentrations, and the activity could be related to interaction with tubulin at the colchicine binding site. Interaction of selected derivatives with tubulinwas evaluated using molecular modeling,...
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Development of potent and effective SARS-CoV-2 main protease inhibitors based on maleimide analogs for the potential treatment of COVID-19
PublicationIn the present work, we report a new series of potent SARS-CoV-2 Main Protease (Mpro) inhibitors based on maleimide derivatives. The inhibitory activities were tested in an enzymatic assay using recombinant Mpro (3CL Protease from coronavirus SARS-CoV-2). Within the set of new Mpro inhibitors, 6e demonstrated the highest activity in the enzymatic assay with an IC50 value of 8.52 ± 0.44 mM. The IC50 value for Nirmatrelvir (PF-07321332,...
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Nutritional and Pharmaceutical Properties of Bioactive Compounds in Organic and Conventional Growing Kiwifruit
PublicationThe bioactivity of two kiwifruit’s cultivars growing under organic and conventional conditions were studied and compared. The bioactive compounds were extracted with water and ethanol using similar conditions which are applied in pharmaceutical applications and for daily fruit consumption such as tea drink. Antioxidant radical scavenging assays [ferric-reducing/antioxidant power (FRAP); cupric reducing antioxidant capacity (CUPRAC);...
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Application of analytical methods for the determination of bioactive compounds in some berries
PublicationFluorometry, ESI-MS, FTIR, and radical scavenging assays were used for characterization of bioactive compounds and the levels of their antioxidant activities. Polyphenols, flavonoids, anthocyanins, and ascorbic acid and the level of antioxidant activity of water extracts of “Murtilla-like” [Myrteola nummularia (Poiret) Berg.], and other widely consumed berries were determined and compared. The contents of bioactive compounds and...
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A convenient and efficient alfa-sulfenylation of carbonyl compounds
PublicationA method for alfa-sulfenylation of carbonyl compounds by a 5,5-dimethyl-2-thioxo-1,3,2-dioxaphosphorinane-2-disulfanyl derivatives has been developed. Readily available reagents, mild reaction conditions, and excellent yields with high selectivity makes this method quite simple, convenient and practical.
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Solving Boundary Value Problems for Second Order Singularly Perturbed Delay Differential Equations by ε-Approximate Fixed-Point Method
PublicationIn this paper, the boundary value problem for second order singularly perturbed delay differential equation is reduced to a fixed-point problem v = Av with a properly chosen (generally nonlinear) operator A. The unknown fixed-point v is approximated by cubic spline vh defined by its values vi = vh(ti) at grid points ti, i = 0, 1, ... ,N. The necessary for construction the cubic spline and missing the first derivatives at the boundary...