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Search results for: controlled drug delivery
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C-1311 (Symadex), a potential anti-cancer drug, intercalates into DNA between A and G moieties. NMR-derived and MD-refined stereostructure of the d(GAGGCCTC) 2 :C-1311 complex
PublicationImidazoacridinone C-1311 (Symadex®) is an antitumor agent which has been recommended for Phase II clinical trials a few years ago. Previously, it was shown experimentally that during the initial stage of its action C-1311 forms stable intercalation complexes with DNA duplexes. Herein, a NMR-derived stereostructure of d(GAGGCCTC)2:C-1311 complex was reported. The ligand was found locating itself between A and G moieties, forming...
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In silico design of telomerase inhibitors.
PublicationTelomerase is a reverse transcriptase enzyme involved in DNA synthesis at the end of linear chromosomes. Unlike in most other cells, telomerase is reactivated most cancerous cells and, therefore, has become a promising new anticancer target. Despite extensive research, direct telomerase inhibitors have yet not been introduced to the clinics because of the complexity of this enzyme. Structures of this protein from simple organisms...
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Investigating the disease- modifying properties of sclerotiorin in Alzheimer's therapy using acetylcholinesterase inhibition
PublicationAlzheimer's disease (AD) is a progressive neurodegenerative disorder caused due to the damage and loss of neurons in specific brain regions. It is the most common form of dementia observed in older people. The symptoms start with memory loss and gradually cause the inability to speak and do day-to-day activities. The cost of caring for those affected individuals is huge and is probably beyond most developing countries capability....
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A Prospective, Randomized, Double-Blind, Parallel-Group, Placebo-Controlled Study Evaluating Meniscal Healing, Clinical Outcomes, and Safety in Patients Undergoing Meniscal Repair of Unstable, Complete Vertical Meniscal Tears (Bucket Handle) Augmented with Platelet-Rich Plasma
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Toward mechanosynthesis of diamondoid structures: vii. simple strategy of building atomically perfect spm tip through attachment of c60 molecule to commercial silicon tip by controlled hydrogen atom desorption from tip asperity si(111) silicon surface
PublicationZaproponowano strategię unieruchomienia cząsteczki c60 na ostrzu chandlowego czujnika spm zbudowanego z krzemu. strategia składa się z czterech prostych etapów i prowadzi do ostrza spm o atomowo zdefiniowanej budowie. modelowanie właściwości ostrza sugeruje, że mogło by ono mieć zastosowanie w mechanosyntezie.
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Dendrimers against fungi – A state of the art review
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Metabolic transformation of antitumor acridinone C-1305 but not C-1311 via selective cellular expression of UGT1A10 increases cytotoxic response: implications for clinical use.
PublicationThe acridinone derivates C-1305 and C-1311 are promising antitumor agents with high activity against several experimental cellular and tumor models and which are under evaluation in pre-clinical and early phase clinical trials. Recent evidence from our laboratories has indicated that both compounds were conjugated by several UGT isoforms with the most active being extrahepatic UGT1A10. The present studies were designed to test...
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Photodynamic therapy of cancer with liposomal photosensitizers
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FROM HARVESTING TO DISTILLATION - EFFECT OF ANALYTICAL PROCEDURES ON THE YIELD AND CHEMICAL COMPOSITION OF RHODODENDRON TOMENTOSUM (LEDUM PALUSTRE) ESSENTIAL OIL
PublicationRhododendron tomentosum possesses the anti-inflammatory, analgesic and antimicrobial properties, determined by the chemical composition of its essential oil. The effects of place (Miszewko, Lubichowo) and time of harvesting (June, November) as well as drying (air-drying, oven-drying, freeze-drying) and isolation (in Deryng, Clevenger and Likens-Nickerson apparatus) procedures on the yield and quality of R. tomentosum essential...
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Budesonide treatment of professional athletes and anti-doping testing- case studies
PublicationAccording to the World Anti-Doping Agency (WADA) Prohibited List, glucocorticosteroids are prohibited in competition and only when administered by oral, intravenous, intramuscular or rectal routes. Up to now, in order to differentiate whether glucocorticosteroids were administered by one of the prohibited routes or not, a specific reporting limit for urinary concentrations of parent compounds and their metabolites was established...
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Human breast milk concentration of neopterin at various stages of lactation and during a single feeding
PublicationThe aim of this work was to determine the physiological level of neopterin in human breast milk, and to study its variability depending on the duration of a single feeding and the lactation stage. Breast milk samples from 74 women were collected between 2 and 4 days after delivery, and at 15, 30, and 90 days after delivery. Additionally, breast milk samples from eight women were collected before and after 7 and 15 min of breastfeeding....
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Screening of predicted synergistic multi-target therapies in glioblastoma identifies new treatment strategies
PublicationAbstract Background IDH-wildtype glioblastoma (GBM) is a highly malignant primary brain tumor with a median survival of 15 months after standard of care, which highlights the need for improved therapy. Personalized combination therapy has shown to be successful in many other tumor types and could be beneficial for GBM patients. Methods We performed the largest drug combination screen to date in GBM, using a high-throughput effort...
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Zwinne wytwarzanie oprogramowania - praktyki wspierane w środowisku IBM Jazz
PublicationW artykule zostało zaproponowane wykorzystanie technologii IBM Jazz w kontekście pracy grupowej proponowanej przez zwinne metodyki takie jak Scrum czy Disciplined Agile Delivery
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INDIRECT CONTROL OVER SUBORDINATE UNITS
PublicationDeveloping a game universe usually involves creation of various units which can be both, encountered by a player or controlled by him. There is a number of works considering autonomous behaviors of units wandering around the game world. When it comes to the units controlled by the player, they are often deprived of autonomy and are strictly controlled by the player. This paper presents a concept of units behavior depending on their...
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Indirect control over subordinate units
PublicationDeveloping a game universe usually involves creation of various units which can be both, encountered by a player or controlled by him. There is a number of works considering autonomous behaviours of units wandering around the game world. When it comes to the units controlled by the player, they often are lack of autonomy and are strictly controlled by the player. This paper presents a concept of units behaviour depending on their...
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New oryginal generic technologies: A Polish R&D strategic implementation programme
PublicationPolands's pharmaceutical industry is of great significance to the whole economy. According to Forbs (2 October 2012), the cost of launching a new drug varies from USD 1 to 11 bilion. There is little Chance of a Polish pharmaceutical company developing an original drug due to financial reason.Many research teams in Poland take up research projects aimed at new biologically active compounds. But such an objective has no broader perspective,...
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Control strategy for the multilevel cascaded H-bridge converter
PublicationThe paper presents the control strategy for Cascaded H-bridge (CHB) converter . The converter output voltage using Space-Vector Pulse Width Modulation (SV-PWM) strategy is controlled. The DC-link voltages are controlled by appropriate choice of H-Bridges and appropriate choice of active and passive vectors.
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Increased cytotoxicity of an unusual DNA topoisomerase II inhibitor compound C-1305 toward HeLa cells with downregulated PARP-1 activity results from re-activation of the p53 pathway and modulation of mitotic checkpoints
PublicationOur previous studies have shown that murine fibroblast cells, in which PARP-1 gene was inactivated by gene disruption, are extremely sensitive to triazoloacridone compound C-1305, an inhibitor of DNA topoisomerase II with unusual properties. Here, we show that pharmacological inhibition of PARP-1 activity by its inhibitor compound NU1025, sensitizes human cervical carcinoma HeLa cells to compound C-1305 compared to treatment with...
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Enhanced Activity of P4503A4 and UGT1A10 Induced by Acridinone Derivatives C-1305 and C-1311 in MCF-7 and HCT116 Cancer Cells: Consequences for the Drugs’ Cytotoxicity, Metabolism and Cellular Response
PublicationActivity modulation of drug metabolism enzymes can change the biotransformation of chemotherapeutics and cellular responses induced by them. As a result, drug-drug interactions can be modified. Acridinone derivatives, represented here by C-1305 and C-1311, are potent anticancer drugs. Previous studies in non-cellular systems showed that they are mechanism-based inhibitors of cytochrome P4503A4 and undergo glucuronidation via UDP-glucuronosyltranspherase...
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A model for agribusiness supply chain risk management using fuzzy logic. Case study: Grain route from Ukraine to Poland
PublicationIn order to establish new logistics routes, it is necessary to address several technical and organizational issues, among others. One of the most important criteria for evaluating the performance of a supply chain is the delivery time, proactive consideration of potential hazards and associated uncertainties that may occur along the route. However, the existing solutions are often passive and reactive, based on statistics, thus...
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Improvement of opipramol base solubility by complexation with β-cyclodextrin
PublicationOpipramol (OPI), a tricyclic antidepressant and anxiolytic compound, is administered orally in the form of a dihydrochloride. Salt form of the drug has a higher solubility in water and hence bioavailability and stability. A similar effect can be achieved by closing the hydrophobic part of the drug molecule in the cyclodextrin cavity. The paper presents opipramol inclusion complexes with beta-cyclodextrin (β-CD) in 1:1 molar ratio....
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A taxonomy of challenges to resilient message dissemination in VANETs
PublicationInter-vehicular communications is seen as a promising solution to a number of issues related with public road safety, road congestion management, and infotainment. However, Vehicular Ad-hoc NETworks (VANETs) characterized by high mobility of vehicles and facing a number of other issues related with high frequency wireless communications and network disconnections, encounter major challenges related with reliability of message delivery....
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Ontology-Aided Software Engineering
PublicationThis thesis is located between the fields of research on Artificial Intelligence (AI), Knowledge Representation and Reasoning (KRR), Computer-Aided Software Engineering (CASE) and Model Driven Engineering (MDE). The modern offspring of KRR - Description Logic (DL) [Baad03] is considered here as a formalization of the software engineering Methods & Tools. The bridge between the world of formal specification (governed by the mathematics)...
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Polyurethanes as a carrier of drugs for gentamicin
PublicationGentamicin is one of the most popular drug and is widely used due to its antibiotic properties. 3% of world production of polyurethanes (PU) is dedicated to biomedical applications, where they can serve are parts of orthopedic prosthesis or artificial organs, disposable medical devices, wound and burn dressing, contact lenses among others. In the study, to obtain drug carriers, a combination of these two materials were prepared...
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Integration and Dependency in Software Lifecycle Based on Jazz Platform
PublicationSoftware delivery organizations are being asked to meet goals that seem mutually exclusive. Teams are asked to increase product quality, accelerate time to market, and meet increasing mandates from regulatory bodies. As software solutions and software development environments become rapidly more complex. Many business drivers compound these challlenges.
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Modeling of pharmaceuticals mixtures toxicity with deviation ratio and best-fit functions models
PublicationThe present study deals with assessment of ecotoxicological parameters of 9 drugs (diclofenac (sodium salt), oxytetracycline hydrochloride, fluoxetine hydrochloride, chloramphenicol, ketoprofen, progesterone, estrone, androstenedione and gemfibrozil), present in the environmental compartments at specific concentration levels, and theirmutual combinations by couples against Microtox® and XenoScreen YES/YAS® bioassays. As the quantitative...
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Overview of DC–DC Converters Dedicated to HVdc Grids
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Estimation of Parameters Associated With Individual Sources of Voltage Fluctuations
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Modified Preisach model of hysteresis in multi air gap ferrite core medium frequency transformer
PublicationThis article presents the modified Preisach model of hysteresis for a 3-phase medium frequency transformer in a 100 kW dual active bridge converter. The transformer magnetic core is assembled out of ferrite I-cores, which results in multiple parasitic air gaps. For this transformer, the hysteresis loops were measured and parameters of the Preisach model were determined. The Preisach distribution function is approximated with a...
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Lagrangian model of an isolated dc-dc converter with a 3-phase medium frequency transformer accounting magnetic cross saturation
PublicationThis article presents a nonlinear equivalent circuit model of an isolated dc-dc converter with a 3-phase medium frequency transformer. The model takes into account the magnetic cross saturation of the 3-phase core-type magnetic circuit. The model is suitable in detailed electromagnetic transient simulations of power systems involving isolated dc-dc converters. The model is developed using the Lagrange energy method. It involves...
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Integration of protein tethering in a rapid and label-free SERS screening platform for drugs of abuse
PublicationSurface enhanced Raman spectroscopy (SERS) has emerged as a promising technique for the rapid and ultrasensitive detection of molecular species such as drugs of abuse in biofluids. Yet, it remains a significant challenge to create a viable screening tool for multiple drug classes, owing to the lack of affinity of certain species for the SERS substrate and to the matrix interference in complex media. Here we report a protein tethering...
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Influence of the electrosynthesis conditions on the spontaneous release of anti-inflammatory salicylate during degradation of polypyrrole coated iron for biodegradable cardiovascular stent
PublicationIn this work, the spontaneous release of anti-inflammatory salicylate from polypyrrole (PPy) coated iron has been studied during degradation of the material in phosphate buffer saline at 37 C. The sodium salicylate was incorporated into PPy in a one-step electropolymerization process. The influence of the synthesis conditions such as sodium salicylate concentration, pyrrole concentration and deposition charge on drug release profile...
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Utilizing Genome-Wide mRNA Profiling to Identify the Cytotoxic Chemotherapeutic Mechanism of Triazoloacridone C-1305 as Direct Microtubule Stabilization
PublicationRational drug design and in vitro pharmacology profiling constitute the gold standard in drug development pipelines. Problems arise, however, because this process is often dicult due to limited information regarding the complete identification of a molecule’s biological activities. The increasing aordability of genome-wide next-generation technologies now provides an excellent opportunity to understand a compound’s diverse eects...
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Supporting First Year Students Through Blended-Learning - Planning Effective Courses and Learner Support
PublicationHigher education has been actively encouraged to find more effective and flaxible delivery models to provide all students with access to good quality learning experiences. This paper describes students opinion about using e-learning techniques and their participation in courses provided in different ways as additional help and expectations of first year students.
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AC Motor Voltage and Audible Noise Dataset
PublicationThe dataset titled AC motor voltage and audible noise waveforms in ship’s electrical drive systems with frequency converters contains the voltage and sound measurement results recorded in a marine frequency controlled AC drive system. The dataset is part of research focussing on the impact of the ship’s electrical drive systems with frequency converters on vibrations and the level of audible noise on ships. The dataset allows the...
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The II phase metabolism of endogenous and exogenous compounds, including antitumor chemotherapeutics
PublicationThe II phase metabolism, it is a set of metabolism and excretion pathways of endogenous as well as exogenous compounds including xenobiotics. UDP-glucuronyltransferases (UGTs; EC 2.4.1.17) are the most crucial representatives of II phase enzymes, which are responsible for the transformation of bilirubine and bile acids, steroids and thyroid hormones and lipids. Exogenous compounds, including drugs, carcinogens, environmental pollutants...
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The transition of HIV within and between affected populations in Poland
PublicationThe aim of the paper is the estimation of probabilities that describe the transition of HIV within and between the following three populations: homosexual and bisexual men, injecting drug users and heterosexual persons in Poland in the years 1995-2006
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Mathemathical model of radial passive magnetic bearing
PublicationIn the article mathematical radial model of passive magnetic bearings to ocean engineering units has been presented. The units application in underwater thrusters should increase propulsion systems durability and gives lower maintenance costs. The rotor of electric motor is hanging in magnetic field taken from radial passive magnetic bearings. However axial direction maintenance must be controlled with electromagnets and their...
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Sensing of anesthetic drugs in blood with Raman spectroscopy
PublicationA proof-of-concept study of a Raman spectroscopy-based approach for measuring the content of anesthesia drugs in blood is presented. Spectra of spiked blood from several patients exhibit prominent changes in regions associated with the drug.
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Stable nanoconjugates of transferrin with alloyed quaternary nanocrystals Ag–In–Zn–S as a biological entity for tumor recognition
PublicationOne way to limit the negative effects of anti-tumor drugs on healthy cells is targeted therapy employing functionalized drug carriers. Here we present a biocompatible and stable nanoconjugate of transferrin anchored to Ag-In-Zn-S quantum dots modified with 11-mercaptoundecanoic acid (Tf-QD) as a drug carrier versus typical anticancer drug, doxorubicin. Detailed investigations of Tf-QD nanoconjugates without and with doxorubicin...
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Applying a Mesoscopic Transport Model to Analyse the Effects of Urban Freight Regulatory Measures on Transport Emissions—An Assessment
PublicationSustainable urban freight management is a growing challenge for local authorities due to social pressures and increasingly more stringent environmental protection requirements. Freight and its adverse impacts, which include emissions and noise, considerably influence the urban environment. This calls for a reliable assessment of what can be done to improve urban freight and meet stakeholders’ requirements. While changes in a transport...
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Electrochemistry meets enzymes: Investigation of the biotransformation pathway of C-1311 based on electrochemical simulation in comparison to in vitro methods.
PublicationThe knowledge of the metabolic pathways and the biotransformation of new drugs is one of the major challenges in pharmaceutical research. It is crucial for elucidation of degradation routes of the new biologically active compounds, especially in the area of possible toxicity. Conventional in vitro drug metabolism studies are based on incubating drug candidate with e.g. hepatocytes or, most importantly, liver cell microsomes and...
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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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Study of Metrological Properties of Voltammetric Electrodes in the Time Domain
PublicationMetrological properties of voltammetric electrodes, in the situation where on their surface an electrochemical reaction of oxidizing/reduction takes place, were analyzed in this chapter. The properties of electrodes on which a reaction controlled by ion transport process takes place were taken into consideration. Also, it was analyzed how the electrode’s shape and the voltage polarizing the electrode influence this electrode’s...
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The overexpression of CPR and P450 3A4 in pancreatic cancer cells changes the metabolic profile and increases the cytotoxicity and pro-apoptotic activity of acridine antitumor agent, C-1748
PublicationDrug resistance is one of the major cause of pancreatic cancer treatment failure. Thus, it is still imperative to develop new active compounds and novel approach to improve drug efficacy. Here we present 9-amino-1-nitroacridine antitumor agent, C-1748, developed in our laboratory, as a candidate for pancreatic cancer treatment. We examined (i) the cellular response of pancreatic cancer cell lines: Panc-1, MiaPaCa-2, BxPC-3 and...
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Metrological analysis of precision of the system of delivering a water capsule for explosive production of water aerosol
PublicationIn this paper an analysis of precision of the system controlling delivery by a helicopter of water-capsule designed for extinguishing large scale fires is presented. The analysis was performed using the numerical method of distribution propagation (Monte Carlo method) supplemented with results of application of the uncertainty propagation method. In addition the optimum conditions for the airdrop are determined to ensure achievement...
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The influence of ILs on TiO2 microspheres activity towards 5-FU removal under artificial sunlight irradiation
PublicationIn this work, the effect of various ionic liquids (ILs), namely, choline chloride [Chol][Cl], hexadecylpyridynium chloride [HDPy][Cl], and tributylmethylammonium chloride [TBMA][Cl], on the morphology, surface compo-sition in relation to photocatalytic oxidation of 5-fluorouracil (5-FU) and phenol in the presence of TiO2 pho-tocatalysts under artificial sunlight conditions was investigated. The highest photoactivity towards cytostatic...
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Quantification of unconjugated and total ibuprofen and its metabolites in equine urine samples by gas chromatography–tandem mass spectrometry: Application to the excretion study
PublicationIbuprofen (IBU) is a widely used nonsteroidal anti-inflammatory drug (NSAID) in human and also veterinary medicine. NSAIDs are usually highly metabolized compounds in horses; they are often present in equine urine, mostly in their conjugated forms (glucuronides). Thus, hydrolysis to cleave the glucuronide linkage prior to anti-doping analysis is often necessary for improving detection. In this study, unconjugated and total IBU...
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Comparative molecular modelling of biologically active sterols
PublicationMembrane sterols are targets for a clinically important antifungal agent – amphotericin B. The relatively specific antifungal action of the drug is based on a stronger interaction of amphotericin B with fungal ergosterol than with mammalian cholesterol. Conformational space occupied by six sterols has been defined using the molecular dynamics method to establish if the conformational features correspond to the preferential interaction...
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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...