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Search results for: fractional derivatives and integrals
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Cytotoxicity of anthraquinone derivatives (Compound 1-9) towards NHBE normal cells
Open Research DataThis study presents absorbance values of formazan product (converted from MTT) which corresponds to the cytotoxicity of anthraquinone derivatives (Compound 1-9) towards NHBE normal cells.
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Cytotoxicity of anthraquinone derivatives (Compound 1-9) towards H460 cancer cell
Open Research DataThis study presents absorbance values of formazan product (converted from MTT) which corresponds to the cytotoxicity of anthraquinone derivatives (Compound 1-9) towards H460 cancer cells.
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Cytotoxicity of anthraquinone derivatives (Compound 1-9) towards A549 cancer cells
Open Research DataThis study presents absorbance values of formazan product (converted from MTT) which corresponds to the cytotoxicity of anthraquinone derivatives (Compound 1-9) towards A549 cancer cells.
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Design and synthesis of new analogues of batracylin linked to tuftsin and retro-tuftsin derivatives
PublicationThe synthesis of derivatives of batracylin with several peptides was elaborated followed by their cytotoxic activity investigation.
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Two-Rate Based Low-Complexity Variable Fractional-Delay FIR Filter Structures
PublicationThis paper considers two-rate based structures for variable fractional-delay (VFD) finite-length impulse response (FIR) filters. They are single-rate structures but derived through a two-rate approach. The basic structure considered hitherto utilizes a regular half-band (HB) linear-phase filter and the Farrow structure with linear-phase subfilters. Especially for wide-band specifications, this structure is computationally efficient...
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Nonlocal three-dimensional theory of elasticity for buckling behavior of functionally graded porous nanoplates using volume integrals
PublicationIn this paper, the buckling of rectangular functionally graded (FG) porous nanoplates based on threedimensional elasticity is investigated. Since, similar researches have been done in two-dimensional analyses in which only large deflections with constant thickness were studied by using various plate theories; therefore, discussion of large deformations and change in thickness of plates after deflection in this study is examined....
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Influence of a lipid bilayer on the conformational behavior of amphotericin B derivatives - A molecular dynamics study.
PublicationAmphotericin B (AmB) is an effective but very toxic antifungal antibiotic. In our laboratory a series of AmB derivatives of improved selectivity of action was synthesized and tested. To understand molecular basis of this improvement, comparative conformational studies of amphotericin B and its two more selectivederivatives were carried out in an aqueous solution and in a lipid membrane. These molecular simulation studies revealed...
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Diaryl Sulfide Derivatives as Potential Iron Corrosion Inhibitors: A Computational Study
PublicationThe present work aimed to assess six diaryl sulfide derivatives as potential corrosion inhibitors. These derivatives were compared with dapsone (4,4′-diaminodiphenyl sulfone), a common leprosy antibiotic that has been shown to resist the corrosion of mild steel in acidic media with a corrosion efficiency exceeding 90%. Since all the studied compounds possess a common molecular backbone (diphenyl sulfide), dapsone was taken as the...
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Investigations on the immunosuppressive activity of derivatives of mycophenolic acid in immature dendritic cell
PublicationThe main activity of mycophenolic acid (MPA) and its analogs is the inhibition of proliferation of T cells. Here, we hypothesized that MPA and its conjugates inhibits also the activity of antigen-presenting cells (APC) including dendritic cells (DCs). We tested the effect of novel amino acid derivatives of MPA and conjugates of MPA with acridines/acridones on DCs by flow cytometry, ELISA and MLR assay. Both acridines/acridone derivatives...
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Novel amides of mycophenolic acid and some heterocyclic derivatives as immunosuppressive agents
PublicationThe group of new amide derivatives of mycophenolic acid (MPA) and selected heterocyclic amines was synthesised as potential immunosuppressive agents functioning as inosine-5'-monophosphate dehydrogenase (IMPDH) uncompetitive inhibitors. The synthesis employed uronium-type activating system (TBTU/HOBt/DIPEA) while or phosphonic acid anhydride method (T3P/Py) facilitating amides to be obtained in moderate to excellent yields without...
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NUMERICAL ESTIMATION OF HULL HYDRODYNAMIC DERIVATIVES IN SHIP MANOUVERING PREDICTION
PublicationOperating in crowded waterways pose a risk of accidents and disasters due to maneuvering limitations of the ship. In order to predict ship’s maneuvering characteristics at the design stage, model tests are often executed as the most accurate prediction tool. Two approaches can be distinguished here: free running model tests and numerical simulations based on planar motion model with the use of hydrodynamic derivatives obtained...
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Synthesis and biological activity of mycophenolic acid-amino acid derivatives
PublicationIn 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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Effect of C-1748 derivatives on the morphological transformation of C. albicans ATCC 10231 cells
Open Research DataThe datasets contain the results of the impact of five C-1748 derivatives (IKE28 - IKE32) on morphological transformation of Candida albicans strain ATCC 10231 cells. Photographic documentation prepared with the TECAN Spark 10M titration plate reader.
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Effect of C-1748 derivatives on the biofilm formation of C. albicans ATCC 10231 cells
Open Research DataThe datasets contain the results of the impact of five C-1748 derivatives (IKE28 - IKE32) on the biofilm formation of Candida albicans strain ATCC 10231 cells. Photographic documentation prepared with the TECAN Spark 10M titration plate reader.
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Amphotericin B and Its New Derivatives - Mode of Action
PublicationAmphotericin B (AmB) is a well known antifungal and antiprotozoal antibiotic used in the clinic for several decades. Clinicalapplications of AmB, however, are limited by its nephrotoxicity and many other acute side effects which are not acceptable by patientswhen their life is not threaten. In order to improve the therapeutic index of this drug, lipid formulations have been introduced and manyefforts have been made to obtain less...
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N-Alkyl Derivatives of L-Glutamine As Inhibitors of Glutamine - Utilizing Enzymes
PublicationA general facile method to synthesize the N-gamma-alkyl and N-gamma,N-gamma-dialkyl derivatives of L-glutamine (1a-d) from L-glutamic acid as a starting substrate is presented. The obtained compounds are shown to inhibit three diferent glutamine-utilizing enzymes, namely: glutaminase, gamma-glutamyl transpeptidase, and glucosamine-6-phosphate synthase, with inhibitory constants within the milimolar range.
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Study of proapoptotic activity of anthraquinone derivatives towards H226 cancer cells using flow cytometry
Open Research DataThis study presents the fluorescence intensity of Annexin V/7AAD and caspase 3/7 which correspond to the proapoptotic activity of anthraquinone derivatives towards H226 cancer cells.
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Study of proapoptotic activity of anthraquinone derivatives towards A549 cancer cells using flow cytometry
Open Research DataThis study presents the fluorescence intensity of Annexin V/7AAD and caspase 3/7 which correspond to the proapoptotic activity of anthraquinone derivatives towards A549 cancer cells.
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Synthesis of bicoumarin thiophosphate derivatives as steroid sulfatase inhibitors
PublicationBased on the frameworks of 7-hydroxy-2,3-dihydro-1H-cyclopenta[c]chromen-4-one, 3-hydroxy- 7,8,9,10-tetrahydro-6H-benzo[c]chromen-6-one and 3-hydroxy-8,9,10,11-tetrahydro-7H-cyclohepta[c] chromen-6-one, a series of bicoumarin thiophosphate analogs have been synthesized and biologically evaluated. Additionally, their binding modes have been modeled using docking techniques. The inhibitory properties of the synthesized compounds...
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Stability of Discrete Fractional Order State-space Systems
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Comparison and validation of integer and fractional order ultracapacitor models
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Time domain validation of ultracapacitor fractional order model
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Diffusion process modeling by using fractional-order models
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Fractional Delay Filter Design for Sample Rate Conversion
PublicationRosnąca liczba różnych standardów szybkości próbkowania stwarza potrzebę stosowania algorytmów konwersji szybkości próbkowania ciągów dyskretnych. Jeżeli współczynnik przepróbkowania nie jest wyrażony jako stosunek małych liczb całkowitych albo gdy nie jest on stały, to rozwiązaniem może być użycie filtrów ułamkowoopóźniających. Umożliwiają one realizację przepróbkowania z dowolną krotnością. Dokładność przepróbkowania algorytmów...
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Fractional Delay Filter Design with Extracted Window Offsetting
PublicationW pracy przedstawiono koncepcję projektowania filtrów ułamkowoopóźniających (FD) bazującą na metodzie okien. W zaproponowanym podejściu w projektowaniu jest używane okno wyodrębnione z odpowiedzi impulsowej filtru optymalnego offsetowanego o opóźnienie ułamkowe projektowanego filtru. Poszczególne filtry FD zaprojektowany w ten sposób nie są optymalnymi filtrami FD, jednak oferują lepszą jakość w zastosowaniu do zmiany szybkości...
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General, Mild, and Metal-Free Functionalization of Indole and Its Derivatives Through Direct C3-Selenylation
PublicationA very mild method for the introduction of functionalized alkylselenyl group at C-3 position of the indole ring was developed. The proposed procedure consists of an electrophilic substitution of indole and its derivatives with bis(O,O-diisopropoxyphosphorothioyl) diselenide and subsequent cleavage of the P–Se bond with tetrabutylammonium fluoride in the presence of various electrophilic reagents. This method can be successfully...
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Reactivity of triphosphinoboranes towards H3B·SMe2: access to derivatives of boraphosphacycloalkanes with diverse substituents
PublicationTriphosphinoboranes activated the B–H bond in the BH3 molecule without any catalysts at room temperature. Hydroboration reactions led to boraphosphacyloalkanes with diverse structures. The outcomes of reactions depend on the size of the phosphanyl substituent on the boron atom of the parent triphosphinoborane, where derivatives of boraphosphacyclobutane and boraphosphacyclohexane were obtained. Furthermore, the precursor of triphosphinoboranes,...
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Synthesis and antimicrobial activity of 6-sulfo-6-deoxy-D-glucosamine and its derivatives
Publication6-Sulfo-6-deoxy-D-glucosamine (GlcN6S), 6-sulfo-6-deoxy-D-glucosaminitol (ADGS) and their N-acetyl and methyl ester derivatives have been synthesized and tested as inhibitors of enzymes catalyzing reactions of the UDP-GlcNAc pathway in bacteria and yeasts. GlcN6S and ADGS at micromolar concentrations inhibited glucosamine-6-phosphate (GlcN6P) synthase of microbial origin. The former was also inhibitory towards fungal GlcN6P N-acetyl...
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Synthesis and antiproliferative activity of new mycophenolic acid conjugates with adenosine derivatives
PublicationNew conjugates of mycophenolic acid (MPA) and adenosine derivatives were synthesized and assessed as potential immunosuppressants on Jurkat cell line and peripheral blood mononuclear cells (PBMC) from healthy donors. As compared to MPA, all compounds were found to be more active against Jurkat cell line. The antiproliferative activities were compared with MPA and adenosine, in both 2′,3′-O-isopropylidene protected and free hydroxyl...
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Synthesis of disubstituted 1,3,4,9-tetrahydropyrano-[3,4-b]indole-1-acetic acids derivatives
Publication1,3,4,9-tetrahydropyrano[3,4-b ]indole-1-acetic acid derivatives are of interest for pharmaceutical research as a core structure for synthesis of biological active substance - Etodolac (selective Cyclooxygenase-2 inhibitor, which belongs to the Non-steroidal Anti-inflammatory Drug, NSAID, that shows a clin-ically effective analgesic and anti-inflammatory activity). Here the way of synthesis of two 1,3,4,9-tetrahydropyrano[3,4-b...
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Sensorless IPMSM drive with rotor position estimator based on analysis of phase current derivatives
PublicationThis paper describes a sensorless Interior Permanent Magnet Synchronous Motor (IPMSM) drive designed for traction applications. Wide-speed sensorless operation is provided with the use of three methods of rotor position estimation designed for: a standstill, low- and high-speed range. The paper focuses on the high-speed estimation algorithm. The estimator uses the derivatives of motor phase currentsresulting from PWM modulation...
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Monosubstituted hydrazone β-cyclodextrin derivatives for pH-sensitive complex formation with aromatic drugs
PublicationA new and convenient synthetic pathway was developed to produce monosubstituted cyclodextrins with high yields. Each of the β-cyclodextrin derivatives described in this work has an aromatic substituent connected with cyclodextrin core by a pH-sensitive hydrazone linker and a carbon chain. Carbon chains differ in lengths having one or three carbon atoms. The correlation between water solubility and linker length was determined using...
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Determination of the minimum inhibitory concentration of C-1305 derivatives (IKE1-IKE8) against Candida strains
Open Research DataThe datasets contain the results of determining the minimum inhibitory concentration of acridone derivatives against C. albicans ATCC 10231, C. glabrata ATCC 90030, C. krusei ATCC 6258 and C. parapsilosis ATCC 22019 by the modified M27-A3 specified by the CLSI.
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IPMSM rotor position estimator based on analysis of phase current derivatives
PublicationThis paper describes an algorithm for estimation of IPMSM angular rotor position. The algorithm uses derivatives of motor phase currents resulting from PWM modulation to obtain the rotor position. The presented method is designed for medium- and high-speed range, since it is based on determination of the EMF vector. Algorithm is characterised by a very simple formulae. The calculation of rotor position is performed in every PWM...
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Synthesis and antiproliferative activity of conjugates of adenosine with muramyl dipeptide and nor-muramyl dipeptide derivatives
PublicationWe synthesized a series of MDP(D,D) and nor-MDP(D,D) derivatives conjugated with adenosine through a spacer as potential immunosuppressants. New conjugates were evaluated on two leukemia cell lines (Jurkat and L1210) and PBMC from healthy donors.
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Biochemical, Structural Analysis, and Docking Studies of Spiropyrazoline Derivatives
PublicationIn this study, we evaluated the antiproliferative potential, DNA damage, crystal struc‐ tures, and docking calculation of two spiropyrazoline derivatives. The main focus of the research was to evaluate the antiproliferative potential of synthesized compounds towards eight cancer cell lines. Compound I demonstrated promising antiproliferative properties, especially toward the HL60 cell line, for which IC50 was equal to 9.4 μM/L....
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Synthesis and biological activity of ester derivatives of mycophenolic acid and acridines/acridones as potential immunosuppressive agents
PublicationImproved derivatives of mycophenolic acid (MPA) are necessary to reduce the frequency of adverse effects, this drug exerts in treated patients. In this study, MPA was coupled with N-(x-hydroxyalkyl)-9-acridone-4-carboxamides or N-(x-hydroxyalkyl)acridine-4-carboxamides to give respective ester conjugates upon Yamaguchi protocol. This esterification required protection of phenol group in MPA. Designed conjugates revealed higher...
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Efficient synthesis and antifungal investigation of nucleosides’ quaternary ammonium salt derivatives
PublicationQuaternary ammonium salts are a group of compounds with diverse biological properties, the most important of which are their antiviral, antibacterial, and antifungal activities. The quaternization reactions of 5'-O-tosyl derivatives of uridine and thymidine with triethylamine, trimethylamine, 4-(N ,N -dimethylamino)pyridine, 2-methylpyridine, and pyridine are described in this article. Two of the synthesized compounds are exceptional...
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Molecular modeling and evaluation of novel dibenzopyrrole derivatives as telomerase inhibitors and potential drug for cancer therapy
PublicationDuring previous years, many studies on synthesis, as well as on anti-tumor, anti-inflammatory and anti-bacterial activities of the pyrazole derivatives have been described. Certain pyrazole derivatives exhibit important pharmacological activities and have proved to be useful template in drug research. Considering importance of pyrazole template, in current work the series of novel inhibitors were designed by replacing central...
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Determination of the minimum inhibitory concentration of C-1330 derivatives (IKE9-IKE14) against Candida strains
Open Research DataThe datasets contain the results of determining the minimum inhibitory concentration of C-1330 derivatives (IKE9-IKE14) against C. albicans ATCC 10231, C. glabrata ATCC 90030, C. krusei ATCC 6258 and C. parapsilosis ATCC 22019 by the modified M27-A3 specified by the CLSI.
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Improvement of time difference of arrival measurements resolution by using fractional delay filters in a direct sequence-code division multiple access radionavigation system
PublicationThis study presents a method of improving time measurements resolution in a direct sequence-code division multiple access receiver by using a fine code tracking loop based on fractional delay filtering of a despreading sequence. It briefly describes the structure of a generic digital code tracking loop and the proposed modification which allows to measure time difference of arrival values with the subsample resolution, together...
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The absorption and fluorescence spectra of C-1305 derivatives (IKE1-IKE8), potential antifungal agents
Open Research DataOptical measurements of C-1305 derivatives (IKE1-IKE8). The absorption spectra were recorded at 300 - 800 nm for solutions with 16 μg / mL derivative concentration. The fluorescence emission spectra were determined at 420-800 nm with the excitation wavelengths 360 or 415 nm for solutions with 1 μg / mL derivative concentration. All measurements were...
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Targeting yeast topoisomerase II by imidazo and triazoloacridinone derivatives resulting in their antifungal activity
PublicationFungal pathogens are considered as serious factors for deadly diseases and are a case of medical concern. Invasive fungal infections also complicate the clinical course of COVID-19, leading to a significant increase in mortality. Furthermore, fungal strains' multidrug resistance has increased the demand for antifungals with a different mechanism of action. The present study aimed to identify antifungal compounds targeting yeast...
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Linear and Nonlinear Optical Properties of Azobenzene Derivatives Modified with an (Amino)naphthalene Moiety
PublicationThe design of two-photon absorbing azobenzene (AB) derivatives has received much attention; however, the two-photon absorption (2PA) properties of bis-conjugated azobenzene systems are relatively less explored. Here, we present the synthesis of six azobenzene derivatives and three bisazobenzenes substituted (or not) at para position(s) with one or two amino group(s). Their linear and nonlinear absorption properties are studied...
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CHITOSAN-DERIVATIVES IN COMBINATIONS WITH SELECTED PORPHYRINOIDS AS NOVEL HYBRID MATERIALS FOR MEDICINE AND PHARMACY
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Chemosensitization of multidrug resistant Candida albicans by the oxathiolone fused chalcone derivatives
PublicationThree structurally related oxathiolone fused chalcone derivatives appeared effective chemosensitizers, able to restore in part sensitivity to fluconazole of multidrug-resistant C.albicans strains. Compound 21 effectively chemosensitized cells resistant due to the overexpression of the MDR1 gene, compound 6 reduced resistance of cells overexpressing the ABC-type drug transporters CDR1/CDR2 and derivative 18 partially reversed fluconazole...
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Effect of chemical structure on complexation efficiency of aromatic drugs with cyclodextrins: The example of dibenzazepine derivatives
PublicationIt is widely believed that the hydrophobic effect governs the binding of guest molecules to cyclodextrins (CDs). However, it is also known that high hydrophobicity of guest molecules does not always translate to the formation of stable inclusion complexes with CDs. Indeed, a plethora of other factors can play a role in the efficiency of guest–CD interactions, rendering structure-based prediction of the complexation efficiency with...
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Application of the Fractional Fourier Transform for dispersion compensation in signals from a fiber-based Fabry-Perot interferometer
PublicationOptical methods of measurement do not require contact of a probe and the object under study, and thus have found use in a broad range of applications such as nondestructive testing (NDT), where noninvasive measurement is crucial. Measuring the refractive index of a material can give a valuable insight into its composition. Low‑coherence radiation sources enable measurement of the sample’s properties across a wide spectrum, while...
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Thermal Decomposition of Carbamoyl Meldrum’s Acids: A Starting Point for the Preparation of 1,3-Oxazine Derivatives
PublicationThe ability to undergo [4 + 2] versus [2 + 2] cycloaddition was under investigation for ketenes thermally generated from carbamoyl Meldrum’s acid. Usually, 1,3-oxazino-5-carbamoylo-4,6-diones are formed when carbamoyl Meldrum’s acid reacts with imine. However, in some cases, a reaction takes an unexpected course, leading to the formation of tetraponerines alkaloids derivatives or cyclic iminoethers.
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Tetrahydroquinolinone derivatives exert antiproliferative effect on lung cancer cells through apoptosis induction
PublicationThe anticancer properties of quinolones is a topic of interest among researchers in the scientific world. Because these compounds do not cause side effects, unlike the commonly used cytostatics, they are considered a promising source of new anticancer drugs. In this work, we designed a brief synthetic pathway and obtained a series of novel 8-phenyltetrahydroquinolinone derivatives functionalized with benzyl-type moieties at position...