Josef Jampilek

Josef Jampilek

Professor of Medicinal Chemistry

About

419
Publications
85,012
Reads
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6,986
Citations
Additional affiliations
May 2022 - present
Cracow University of Technology
Position
  • visiting professor
Description
  • Drug Design & Discovery, Specific Modifications of Drugs
November 2021 - November 2021
Wroclaw Medical University
Position
  • Professor
Description
  • Bioavailability of drugs
October 2019 - October 2019
University of Macau
Position
  • Professor
Description
  • Drug Design & Discovery, Specific Modifications of Drugs: Prodrugs, Bioprecursors, and Soft and Hard Drugs
Education
March 2016 - May 2017
Comenius University Bratislava
Field of study
  • Medicinal Chemistry
October 2006 - March 2009
University of Veterinary and Pharmaceutical Sciences Brno, Faculty of Pharmacy
Field of study
  • Medicinal Chemistry
September 2000 - April 2004
Charles University, Faculty of Pharmacy
Field of study
  • Medicinal Chemistry

Publications

Publications (419)
Chapter
Medicinal plants have been used around the world in folk medicine for generations since ancient times, and today people enjoy using these natural medicines for their healing properties, with some of their pharmacologically active phytoconstituents recently serving as a lead for new drug development. Numerous aromatic plants producing aromatic secon...
Chapter
Fungicides are compounds of chemical (organic and inorganic compounds) or biological (i.e., microorganisms, plant root exudates, microbial enzymes) origins that are able to prevent, inhibit or control fungal pathogens or their spores and are used against harmful fungi causing severe plant diseases, which are responsible for pronounced losses of cro...
Chapter
Anthropogenic agricultural and industrial activities resulted in the global degradation of large areas, whereby the overuse of agrochemicals due to low nutrient use efficiency by crops since the mid-twentieth century contributed to a pronounced decline in agricultural soil fertility, resulting in deficiency of some essential nutrients needed for he...
Cover Page
Full-text available
We accepted invitations to serve as Guest Editors for a Special Issue of the journal /Molecules/ (https://www.mdpi.com/journal/molecules/about) on the subject of “Chromatography and Spectrometry in Food Safety and Pharmaceutical Analysis". It is our pleasure to invite you to submit a *Review or Research article* on this topic. We would appreciate y...
Article
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In this paper, we describe a new method for synthesizing hybrid combinations of 1,2,3-triazoles with a tetracyclic quinobenzothiazinium system. The developed approach allowed for the production of a series of new azaphenothiazine derivatives with the 1,2,3-triazole system in different positions of the benzene ring. In practice, the methodology cons...
Article
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This study aimed to obtain and investigate ZnCr2Se4 single crystals doped with rhenium. The single crystals were obtained by applying chemical vapour transport. An X-ray study confirmed the cubic (Fd3¯m) structure of the tested crystals. Thermal, magnetic, electrical, and specific heat measurements accurately determined the physicochemical characte...
Chapter
Due to the rapidly increasing human population and ongoing climate change, modern smart agriculture management is essential for the production of sufficient healthy food, enabling to achieve high yields of crops with improved nutritional quality at low costs and minimizing contamination of environmental matrices with compounds without adverse impac...
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Bioactive calcium phosphate ceramics (CaPs) are one of the building components of the inorganic part of bones. Synthetic CaPs are frequently used as materials for filling bone defects in the form of pastes or composites; however, their porous structure allows modification with active substances and, thus, subsequent use as a drug carrier for the co...
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Twelve drugs containing sildenafil compounds (sildenafil citrate and sildenafil base) were examined using X-ray studies and thermal analysis. According to the manufacturer’s information, the presence of sildenafil was confirmed in all investigated drugs. The positions of diffraction lines (value of 2θ angle) agree with the patterns presented in the...
Article
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Conventional intake of drugs and active substances is most often based on oral intake of an appropriate dose to achieve the desired effect in the affected area or source of pain. In this case, controlling their distribution in the body is difficult, as the substance also reaches other tissues. This phenomenon results in the occurrence of side effec...
Article
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The antitumor potency of a series of designed and prepared antibacterial quinobenzothiazines was evaluated against different types of human cancer cell lines, such as glioblastoma SNB-19, lung adenocarcinoma A549 and breast cancer T47D, and the activities of the compounds were compared to cisplatin and doxorubicin. 9-Propoxy-5-methyl-12H-quino[3,4-...
Article
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Although it may not seem like it, chemical biology has existed for a long time from today’s perspective [...]
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A series of seventeen 4-chlorocinnamanilides and seventeen 3,4-dichlorocinnamanilides were characterized for their antiplasmodial activity. In vitro screening on a chloroquine-sensitive strain of Plasmodium falciparum 3D7/MRA-102 highlighted that 23 compounds possessed IC50 < 30 µM. Typically, 3,4-dichlorocinnamanilides showed a broader range of ac...
Chapter
Plant diseases caused by viruses, bacteria, fungi and nematodes significantly reduce crop yields globally, and effective management strategies are therefore urgently needed. Due to the increasing resistance of phytopathogens to many widely used, especially synthetic pesticides, research into effective antimicrobials suitable for the control of plan...
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This study aimed to evaluate the lipophilicity of a series substances lowering the concentration of uric acid in blood and anti-androgen drugs by thin-layer chromatography in reversed-phase systems (RP-TLC, RP-HPTLC) and computational methods. The chromatographic parameter of lipophilicity (RMW) of tested compounds was determined on three stationar...
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According to the WHO, cancer caused almost 10 million deaths worldwide in 2020, i.e., almost one in six deaths. Among the most common are breast, lung, colon and rectal and prostate cancers. Although the diagnosis is more perfect and spectrum of available drugs is large, there is a clear trend of an increase in cancer that ends fatally. A major adv...
Article
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A new method for modifying the structure of tetracyclic quinobenzothiazinium derivatives has been developed, allowing introduction of various substituents at different positions of the benzene ring. The method consists of reacting appropriate aniline derivatives with 5,12-(dimethyl)thioquinantrenediinium bis-chloride. A series of new quinobenzothia...
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The use of natural compounds is becoming increasingly popular among patients, and there is a renewed interest among scientists in nature-based bioactive agents. Traditionally, herbal drugs can be taken directly in the form of teas/decoctions/infusions or as standardized extracts. However, the disadvantages of natural compounds, especially essential...
Article
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A series of thirty-two anilides of 3-(trifluoromethyl)cinnamic acid (series 1) and 4-(trifluoromethyl)cinnamic acid (series 2) was prepared by microwave-assisted synthesis. All the compounds were tested against reference strains Staphylococcus aureus ATCC 29213 and Enterococcus faecalis ATCC 29212 and resistant clinical isolates of methicillin-resi...
Article
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The knowledge of interactions between different molecules is undoubtedly the driving force of all contemporary biomedical and biological sciences. Chemical biology/biological chemistry has become an important multidisciplinary bridge connecting the perspectives of chemistry and biology to the study of small molecules/peptidomimetics and their inter...
Book
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https://www.elsevier.com/books/bacterial-physiology-and-biochemistry/kushkevych/978-0-443-18738-4 Bacterial Physiology and Biochemistry provides the most current, authoritative, and relevant presentation of bacterial physiology and biochemistry on subject, chemical composition and functional bacterial cell structure, nutrition and growth, the proc...
Conference Paper
Full-text available
Recently, a series of thirty-eight 4-{[(benzyloxy)carbonyl]amino}-2-hydroxybenzoic acid amides designed as potential acetyl- and butyrylcholinesterase (AChE/BChE) inhibitors were described as potential drugs to alleviate the symptoms of Alzheimer’s disease (AD). Some of these compounds have shown promise for inhibiting either AChE or BChE. Since th...
Conference Paper
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A series of twenty-two monosubstituted N-aryl-4-hydroxyquinoline-3-carboxanilides designed as dual anti-invasive agents was prepared and characterized. Lipophilicity significantly affects biological activities of compounds and ADME properties; therefore, the lipo-hydrophilic properties of these 4-hydroxyquinoline-3-carboxanilides were investigated....
Article
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Due to the urgent need of innovation in the antimalarial therapeutic arsenal, a series of thirty-seven ring-substituted N-arylcinnamanilides prepared by microwave-assisted synthesis were subjected to primary screening against the chloroquine-sensitive strain of P. falciparum 3D7/MRA-102. The lipophilicity of all compounds was experimentally determi...
Chapter
High contamination of soils with heavy metals, mainly due to increasing anthropogenic activity, significantly contributed to the reduction of soil fertility worldwide and has an adverse impact on crop production and non-target organ-isms. In addition, toxic metals accumulating in the consumable parts of plants in quantities exceeding permissible le...
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High contamination of soils with heavy metals, mainly due to increasing anthropogenic activity, significantly contributed to the reduction of soil fertility worldwide and has an adverse impact on crop production and non-target organisms. In addition, toxic metals accumulating in the consumable parts of plants in quantities exceeding permissible lev...
Chapter
Fungi are undoubtedly one of the most widespread group organisms on Earth. In addition to their multiple uses in various areas of human activities, fungi produce a wide range of different volatile organic compounds based on hydrocarbons, alcohols, phenols, amines, carbonyl and carboxyl derivatives and heterocycles. These volatile organic compounds...
Article
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A series of eleven benzylated intermediates and eleven target compounds derived from salicylanilide were tested against Staphylococcus aureus ATCC 29213 and Enterococcus faecalis ATCC 29212 as reference strains and against three clinical isolates of methicillin-resistant S. aureus (MRSA) and three isolates of vancomycin-resistant E. faecalis. In ad...
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Emulsions are traditionally used as galenic forms for the local or systemic delivery of drugs and nutritional supplements. They are also used in cosmetics. In the 21st century, there is no area where nanotechnology does not intervene, so nanoemulsions have been prepared and characterized. This new generation of delivery forms can better protect act...
Article
Gold nanoparticles were prepared by the method of chemical reduction utilising sodium borohydride as reducing agent and stabilised with bisammonium gemini surfactants with variable length of polymethylene spacer. Physico-chemical investigations indicated the presence of plasmon resonance peaks in the wavelength range 507 – 544 nm for all investigat...
Article
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Monocrystalline chalcogenide spinels ZnCr2Se4 are antiferromagnetic and semiconductor materials. They can be used to dope or alloy with related semiconducting spinels. Therefore, their Pb-doped display is expected to have unique properties and new potential applications. This paper presents the results of dc and ac magnetic measurements, including...
Article
Introduction: : Some of otherwise useful fungi are pathogenic to humans, and unfortunately, the number of these pathogens is increasing. In addition to common skin infections, these opportunistic pathogens are able to cause severe, often incurable, systemic mycoses. Areas covered: : The number of antifungal drugs is limited, especially drugs tha...
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Viruses can be considered as one of the most common causes of human disease. The human immunodeficiency virus (HIV) causing acquired immunodeficiency syndrome (AIDS) in humans appeared about 40 years ago and is still a major global health problem. On the other hand, during all this time there has been great progress in antiretroviral treatment, whi...
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Excessive use of agrochemicals, including photosystem II (PS II)- inhibiting herbicides, especially after 1950, resulted in significant contamination of environmental matrices. Although some of these photosynthesis-inhibiting herbicides, including atrazine or simazine, have been banned in many countries due to their endocrine disrupting activities,...
Article
Full-text available
Pattern 1-hydroxy-N-(2,4,5-trichlorophenyl)-2-naphthamide and the thirteen original carbamates derived from it were prepared and characterized. All the compounds were tested against Staphylococcus aureus ATCC 29213 as a reference and quality control strain and in addition against three clinical isolates of methicillin-resistant S. aureus (MRSA). Mo...
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Climate change and increasing contamination of the environment, due to anthropogenic activities, are accompanied with a growing negative impact on human life. Nowadays, humanity is threatened by the increasing incidence of difficult-to-treat cancer and various infectious diseases caused by resistant pathogens, but, on the other hand, ensuring suffi...
Chapter
Globally, huge crop yield losses are observed due to soil degradation accompanied by insufficient nutrient content needed for healthy plant development and growth. Therefore, soil or foliar applications of essential metal micronutrients to plants in formulations providing their sustained and controlled release for a longer period are desirable. On...
Article
Infections are a growing global threat, and the number of resistant species of microbial pathogens is alarming. However, the rapid development of cross-resistant or multidrug-resistant strains and the development of so-called ‘superbugs’ are in stark contrast to the number of newly launched anti-infectives on the market. In this review, I summarize...
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Microbial infections caused by a variety of drug-resistant microorganisms are more common , but there are fewer and fewer approved new antimicrobial chemotherapeutics for systemic administration capable of acting against these resistant infectious pathogens. Formulation innovations of existing drugs are gaining prominence, while the application of...
Article
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A series of eighteen 4-chlorocinnamanilides and eighteen 3,4-dichlorocinnamanilides were designed, prepared and characterized. All compounds were evaluated for their activity against gram-positive bacteria and against two mycobacterial strains. Viability on both cancer and primary mammalian cell lines was also assessed. The lipophilicity of the com...
Chapter
Intensification of agriculture over the years was accompanied also with the excessive use of fertilizers and pesticides and monoculture cropping, which caused serious environmental problems reflected in the degradation of soil fertility, environmental pollution, and decline in biodiversity. Considering the increasing human population and ongoing cl...
Article
Full-text available
This research focused on a three-step synthesis, analytical, physicochemical, and biological evaluation of hybrid molecules 6a–g, containing a lipophilic 3-trifluoromethylphenyl moiety, polar carbamoyloxy bridge, 2-hydroxypropan-1,3-diyl chain and 4-(substituted phenyl)-/4-diphenylmethylpiperazin-1-ium-1-yl fragment. The estimation of analytical an...
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X-ray powder diffraction (XRPD) and thermal analysis (differential scanning calorimetry/derivative of thermogravimetry (DSC/DTG)) are solid-state techniques that can be successfully used to identify and quantify various chemical compounds in polycrystalline mixtures, such as dietary supplements or drugs. In this work, 31 dietary supplements availab...
Article
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A series of 1,3,5-triazinyl aminobenzenesulfonamides substituted by aminoalcohol, aminostilbene, and aminochalcone structural motifs was synthesized as potential human carbonic anhydrase (hCA) inhibitors. The compounds were evaluated on their inhibition of tumor-associated hCA IX and hCA XII, hCA VII isoenzyme present in the brain, and physiologica...
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Already at the beginning of the 20th century, the immunomodulatory function of intestinal and gastric bacterial colonies was described. Currently, there is a growing interest in probiotics due to their ability be combined with various drugs to increase/modify the effect of treatment or alleviate the side effects of treatment on the body. Very valua...
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More and more people suffer from a variety of chronic inflammatory diseases, which are mainly caused by stress and a deteriorating environment. Chronic inflammatory bowel diseases are one of the most common such diseases. Their treatment is problematic and lengthy, and in fact, patients are never really cured. In addition, these diseases are associ...
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A series of new tertiary phenothiazine derivatives containing a quinoline and a pyridine fragment was synthesized by the reaction of 1-methyl-3-benzoylthio-4-butylthioquinolinium chloride with 3-aminopyridine derivatives bearing various substituents on the pyridine ring. The direction and mechanism of the cyclization reaction of intermediates with...
Article
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Since the worldwide incidence of bone disorders and cartilage damage has been increasing and traditional therapy has reached its limits, nanomaterials can provide a new strategy in the regeneration of bones and cartilage. The nanoscale modifies the properties of materials, and many of the recently prepared nanocomposites can be used in tissue engin...
Chapter
With a changing climate and cultivation of vast agricultural monocultures, the abundance of various pests shows an increase and their activity is shifting, expanding and intensifying. To avoid losses on crops, a variety of synthetic pesticides are increasingly being used to control harmful pests. This trend leads to overuse of pesticides, which has...
Conference Paper
Full-text available
2-Hydroxy-N-phenylnaphthalene-1-carboxamide, three fluoro monosubstituted and five fluoro disubstituted 2-hydroxynaphthalene-1-carboxanilides were prepared by microwave-assisted synthesis and characterized. All the compounds were evaluated for their ability to inhibit photosynthetic electron transport (PET) in spinach (Spinacia oleracea L.) chlorop...
Conference Paper
Full-text available
Unsubstituted (2E)-N-phenyl-3-[2-(trifluoromethyl)phenyl]prop-2-enamide and six other ortho- or para-halogen-substituted anilides of 2-(trifluoromethyl)cinnamic acid were prepared. As the benzene nucleus of cinnamic acid itself is substituted in C(2) position with a trifluoromethyl moiety that is spatially close to both the amide bond and the halog...
Conference Paper
Full-text available
Various chronic inflammatory diseases have become a problem, especially in the Western world. Whether it concerns inflammation of visceral organs, joints, bones, etc., it is always a physiological reaction of the body, which always tries to eradicate harmful substances and restore tissue homeostasis. Unfortunately, prolonged or chronic inflammation...
Article
Full-text available
The results presented in this paper confirm the beneficial role of an easy-to-use and low-cost thin-layer chromatography (TLC) technique for describing the retention behavior and the experimental lipophilicity parameter of two biguanide derivatives, metformin and phenformin, in both normal-phase (NP) and reversed-phase (RP) TLC systems. The retenti...
Chapter
Protozoa (unicellular eukaryotes) are wild or parasitic organisms that feed on organic matter, such as other microorganisms or organic tissues and debris. Protozoans have historically been considered “unicellular animals” because they are characterized by animal‐like behaviors such as mobility and predation, and lack the cell wall and photosynthesi...
Chapter
Algae are photosynthetic organisms living in oceans and freshwater lakes and rivers and as primary producers they represent the basic tropical level of the food network in aquatic ecosystems. In addition, they effectively capture atmospheric CO2 and produce about 50% of all oxygen on Earth. On the other hand, marine and freshwater micro- and macro-...
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Metal-based nanoparticles (MNPs) frequently demonstrate physical and chemical properties different from the same bulky materials, and therefore it is important to recognize their potential nano-specific toxicity, which could adversely affect plant growth and development, and monitor the accumulation of toxic metals exceeding the permitted levels in...
Article
Two groups of novel anti-infective agents, 3-hydroxynaphthalene-2-carboxanilides and 2-hydroxynaphthalene-1-carboxanilides, were studied by voltammetric techniques at the glassy carbon electrode in aqueous media. Oxidation of hydroxyl group was observed for all forty-four studied compounds, all of them differentiated by a position and a substituent...
Article
Full-text available
A series of 14 target benzyl [2-(arylsulfamoyl)-1-substituted-ethyl]carbamates was prepared by multi-step synthesis and characterized. All the final compounds were tested for their ability to inhibit acetylcholinesterase (AChE) and butyrylcholinesterase (BChE) in vitro, and the selectivity index (SI) was determined. Except for three compounds, all...
Article
Full-text available
Nature has been a source of inspiration for the development of new pharmaceutically active agents. A series of new unnatural gallotannins (GTs), derived from d-lyxose, d-ribose, l-rhamnose, d-mannose, and d-fructose have been designed and synthesized in order to study the protective and antimicrobial effects of synthetic polyphenols that are struct...
Article
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Recently, there has been great interest in the application of polysaccharides in the preparation of diverse biomaterials which result from their biocompatibility, biodegradability and biological activity. In this work, the investigations on chitosan/poly(aspartic acid)-based hydrogels modified with starch were described. Firstly, a series of hydrog...
Article
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Phosphorus-containing heterocyclic cationic surfactants alkyldimethylphenylphospholium bromides with the alkyl chain length 14 to 18 carbon atoms were used for the stabilization of silver nanodispersions. Zeta potential of silver nanodispersions ranges from +35 to +70 mV, which indicates the formation of stable silver nanoparticles (AgNPs). Long-ch...
Article
Full-text available
A set of twenty-four 3-hydroxynaphthalene-2-carboxanilides, disubstituted on the anilide ring by combinations of methoxy/methyl/fluoro/chloro/bromo and ditrifluoromethyl groups at different positions, was prepared. The compounds were tested for their ability to inhibit photosynthetic electron transport (PET) in spinach (Spinacia oleracea L.) chloro...
Article
Full-text available
The new series of single-crystalline chromium selenides, Ta-doped ZnCr2Se4, was synthesised by a chemical vapour transport method to determine the impact of a dopant on the structural and thermodynamic properties of the parent compound. We present comprehensive investigations of structural, electrical transport, magnetic, and specific heat properti...
Article
Full-text available
A series of twelve nature-inspired 3,4,5-trimethoxycinnamates were prepared and characterized. All compounds, including the starting 3,4,5-trimethoxycinnamic acid, were tested for their ability to inhibit acetylcholinesterase (AChE) and butyrylcholinesterase (BChE) in vitro; the selectivity index (SI) was also determined. 2-Fluororophenyl (2E)-3-(3...
Chapter
Seaweeds, which together with corals create marvelous underwater formations playing with many colors, are photosynthesizing organisms producing significant amount of oxygen in the atmosphere. Therefore, a decline in their populations would result in an adverse impact on the environment. The surface of these marine macroalgae contains various functi...
Chapter
Permanent changes in atmospheric composition and land use due to the anthropogenic activity result in climate change accompanied by frequent extreme weather such as prolonged drought periods or massive rainstorms. The increasing adverse impact of abiotic stresses such as elevated temperature, drought, increased soil salinity or floods, as well as e...
Chapter
The population of our planet is growing rapidly, so it is necessary to ensure the production of the necessary amount of food, but also to focus on extending the shelf life of food without the need to produce “synthetic” food doped with various preservatives and stabilizers. One way to maintain the long-term freshness of food is to use suitable pack...
Article
Full-text available
A library of novel 4-{[(benzyloxy)carbonyl]amino}-2-hydroxybenzoic acid amides was designed and synthesized in order to provide potential acetyl- and butyrylcholinesterase (AChE/BChE) inhibitors; the in vitro inhibitory profile and selectivity index were specified. Benzyl (3-hydroxy-4-{[2-(trifluoromethoxy)phenyl]carbamoyl}phenyl)carbamate was the...
Article
Physico-chemical studies of (Zn1–xDyx)Cr2Se4 and Zn[Cr2–xDyx]Se4 spinel systems (x = 0.05, 0.10) containing dysprosium ions in both tetra- and octahedral positions have shown an enhancement of long-range antiferromagnetic interactions and a weakening of short-range ferromagnetic ones. This resulted in the appearance of geometric type spin-glass in...
Article
Full-text available
Medicinal and aromatic plants have been used by mankind since ancient times. This is primarily due to their healing effects associated with their specific secondary metabolites (some of which are also used as drugs in modern medicine), or their structures, served as a basis for the development of new effective synthetic drugs. One way to increase t...
Article
Full-text available
The synthesis and application of sodium trithiocarbonate (Na2CS3) for the treatment of real galvanic wastewater in order to remove heavy metals (Cu, Cd and Zn) was investigated. A Central Composite Design/Response Surface Methodology (CCD/RSM) was employed to optimize the removal of heavy metals from industrial wastewater. Adequacy of approximated...
Article
Full-text available
Carbon is one of the most abundant elements on Earth. In addition to the well-known crystallographic modifications such as graphite and diamond, other allotropic carbon modifications such as graphene-based nanomaterials and carbon nanotubes have recently come to the fore. These carbon nanomaterials can be designed to help deliver or target drugs mo...
Article
This article has been withdrawn at the request of the author(s) and/or editor. The Publisher apologizes for any inconvenience this may cause. The full Elsevier Policy on Article Withdrawal can be found at https://www.elsevier.com/about/our-business/policies/article-withdrawal
Article
Full-text available
Inflammatory diseases, whether caused by excessive stress on certain tissues/parts of the body or arising from infections accompanying autoimmune or secondary diseases, have become a problem, especially in the Western world today. Whether these are inflammations of visceral organs, joints, bones, or the like, they are always a physiological reactio...