Josef Jampilek

Josef Jampilek

Professor of Medicinal Chemistry

About

387
Publications
69,026
Reads
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5,505
Citations
Additional affiliations
May 2022 - May 2022
Cracow University of Technology
Position
  • invited 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 (387)
Article
Full-text available
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...
Chapter
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...
Chapter
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...
Article
Full-text available
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...
Article
Full-text available
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
Full-text available
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...
Article
Full-text available
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
Full-text available
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...
Chapter
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...
Chapter
Full-text available
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...
Article
Full-text available
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
Full-text available
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...
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-...
Chapter
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
Full-text available
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
Full-text available
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
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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...
Article
Full-text available
Studies carried out by X-ray and thermal analysis confirmed that acetaminophen (paracetamol), declared by the manufacturers as an Active Pharmaceutical Ingredient (API), was present in all studied medicinal drugs. Positions of diffraction lines (2θ angles) of the studied drugs were consistent with standards for acetaminophen, available in the ICDD...
Chapter
The use of nanotechnologies can pronouncedly contribute to sustainable intensification of agricultural production. Beneficial impact of nanoparticles (NPs) used as fertilizers on crops is reflected primarily in higher yields but NPs could positively affect also the quantity and quality of secondary metabolites such as phenolics or flavonoids showin...
Chapter
Water, one of the basic conditions of life on Earth, is becoming more and more polluted. Beside easily mechanically removable waste, water is usually contaminated also with many hazardous xenobiotics, which, thanks to their physico-chemical properties, are able to withstand existing cleaning processes. Untreated water then becomes a part of surface...
Article
Chemical compounds with a general formula CuCr2–xMnxSe4 (x = 0.1, 0.2) were successfully synthesized in polycrystalline form, using solid state reaction method, and as nanoparticles, using high-energy ball milling. The influence of manganese and grain size on their structure, magnetic and thermal properties was investigated by X-ray Diffraction (XR...
Conference Paper
Full-text available
A set of six 3-hydroxynaphthalene-2-carboxanilides, substituted on the anilide ring by combinations of methoxy–methoxy, methoxy–fluoro and methoxy–chloro groups at different positions, was designed. All the molecules were prepared by microwave-assisted synthesis. The compounds were tested for their ability to inhibit photosynthetic electron transpo...
Conference Paper
Full-text available
(2E)-3-(3,4-Dichlorophenyl)-N-arylprop-2-enanilides were designed as potential bioactive agents. Six compounds were mono- and di-chlorinated also on the anilide ring. Since the biological activities of molecules are influenced by lipophilicity, the hydro-lipophilic characteristics of these compounds were experimentally studied. In addition, the ove...
Conference Paper
Full-text available
A series of seven fluorinated benzyl carbamates of 4-aminosalicylanilides and unsubstituted benzyl [3-hydroxy-4-(phenylcarbamoyl)phenyl]carbamate designed as agents with the expected anticholinesterase and anti-inflammatory activity were prepared and characterized. As lipophilicity significantly influences the biological activity of compounds, the...
Article
Full-text available
Nutraceuticals are defined as foods or their extracts that have a demonstrably positive effect on human health. According to the decision of the European Food Safety Authority, this positive effect, the so-called health claim, must be clearly demonstrated best by performed tests. Nutraceuticals include dietary supplements and functional foods. Thes...
Article
Full-text available
Possible use of potassium ferrate(VI) (K2FeO4) for the treatment of landfill leachate (pH = 8.9, Chemical Oxygen Demand (COD) 770 mg O2/L, Total Organic Carbon (TOC) 230 mg/L, Total Nitrogen (Total N) 120 mg/L, Total Phosphorus (Total P) 12 mg/L, Total Coli Count (TCC) 6.8 log CFU/mL (Colony-Forming Unit/mL), Most Probable Number (MPN) of fecal ent...
Article
Full-text available
A series of twenty-two novel N-(disubstituted-phenyl)-3-hydroxynaphthalene- 2-carboxamide derivatives was synthesized and characterized as potential antimicrobial agents. N-[3,5-bis(trifluoromethyl)phenyl]- and N-[2-chloro-5-(trifluoromethyl)phenyl]-3-hydroxy- naphthalene-2-carboxamide showed submicromolar (MICs 0.16-0.68 µM) activity against methi...
Article
Full-text available
A series of nineteen novel ring-substituted N-arylcinnamanilides was synthesized and characterized. All investigated compounds were tested against Staphylococcus aureus as the reference strain, two clinical isolates of methicillin-resistant S. aureus (MRSA), and Mycobacterium tuberculosis. (2E)-N-[3-Fluoro-4-(trifluoromethyl)phenyl]-3-phenylprop-2-...
Article
Full-text available
Ibuprofen is one of the best-known nonsteroidal anti-inflammatory and analgesic drugs. Following the previous work, the current study is focused on estimating the effect of different chromatographic conditions on the sensitivity of thin-layer chromatography in combination with UV densitometry, i.e., the detection and quantification of ibuprofen in...
Article
ZnCr2Se4 spinel single crystals doped with neodymium ions having concentrations of 0.05, 0.08 and 0.10 and occupying tetrahedral positions were synthesized using chemical vapour transport. Thermal analysis as well as electrical conductivity, magnetic isotherm, and magnetic susceptibility measurements showed thermal stability at higher temperatures,...
Chapter
The emerging resistance of Mycobacterium tuberculosis and other so-called nontuberculous mycobacteria to clinically used drugs, including second- and third-choice drugs, and the development of cross-resistant or multidrug-resistant strains are alarming. An increase in the number of these infections and the occurrence of nontuberculous opportunistic...
Chapter
Insects represent the most diverse group of organisms on our planet with approximately one million described species. While some of them have beneficial effects in ecosystem services through plant pollination and natural pest control, there are numerous quarantine insect pests causing considerable damage to crop production and storage. Consequently...
Article
The oncogenic mutated kinase BRAFV600E is an attractive molecular target because it is expressed in several human cancers, including melanoma. To present, only three BRAF small inhibitors are approved by the FDA for the treatment of patients with metastatic melanoma: Vemurafenib, Dabrafenib and Encorafenib. Although many protocol treatments have be...
Article
Silver nanoparticles were prepared by chemical reduction method and stabilised with cationic single-chain phosphonium surfactants of variable alkyl chain length and a different number of methyl and phenyl substituents in the hydrophilic headgroup part of surfactant molecule. Physical properties of silver nanoparticles were studied utilizing several...
Article
3-[4-(Substituted)phenyl-/4-(diphenylmethyl)phenylpiperazin-1-yl]-2-hydroxypropyl-1-[(substituted)phenyl]carbamates and their salts with hydrochloric acid were synthesized, characterized, and tested in vitro against Staphylococcus aureus ATCC 29213 and Enterococcus faecalis ATCC 29212 as reference and quality control strains, against three methicil...
Poster
Full-text available
Gallotaniny jsou polyfenolické sloučeniny skládající se z centrální molekuly cukru, na kterou jsou esterickou vazbou navázány zbytky kyseliny gallové. Vyznačující se řadou farmakologických aktivit jako je cytostatická, antioxidační, antibakteriální, protizánětlivá, anobezická nebo antivirová. Bylo připraveno 8nových gallotaninů odvozených od 1, 2,...
Article
Full-text available
Ring-substituted 1-hydroxynaphthalene-2-carboxanilides were previously investigated for their antimycobacterial properties. In our study, we have shown their antiproliferative and cell death-inducing effects in cancer cell lines. Cell proliferation and viability were assessed by WST-1 assay and a dye exclusion test, respectively. Cell cycle distrib...