Josef Jampilek

Hard bone disease is a clinical problem affecting more than 20 million people annually worldwide, with significant health, social, and economic consequences. For successful integration of any implant, the key aspects are bone regeneration, osseointegration at the bone–implant interface, and the mitigation of inflammation. The purpose of this resear...

Carbon has a unique position among the elements, due to the fact that its valence shell has four electrons and is therefore quadrivalent in the excited state [...]

Restoring the structures and functions of tissues along with organs in human bodies is a topic gathering attention nowadays. These issues are widely discussed in the context of regenerative medicine. Excipients/delivery systems play a key role in this topic, guaranteeing a positive impact on the effectiveness of the drugs or therapeutic substances...

Citation: Zieba, A.; Kozik, V.; Suwinska, K.; Kawulok, A.; Pluta, T.; Jampilek, J.; Bak, A. Synthesis and Structure of 5-Methyl-9-(trifluoromethyl)-12H-quino[3,4-b][1,4]benzothiazinium Chloride as Anticancer Agent. Molecules 2024, 29, 4337. https:// Abstract: In this work, the synthesis, structural analysis and anticancer properties of 5-methyl-9-t...

Since the last decade, silver nanoparticles (AgNPs) continue to attract interest of both academia and industry due to their peculiar physical, chemical, and optical properties. In the field of pharmaceutical applications, they are efficient carriers in the processes of controlled drug release, improve the drug’s bioavailability, act as efficient an...

A series of new unique acetylene derivatives of 8-hydroxy- and 8-methoxyquinoline- 5-sulfonamide 3a–f and 6a–f were prepared by reactions of 8-hydroxy- and 8-methoxyquinoline- 5-sulfonyl chlorides with acetylene derivatives of amine. A series of new hybrid systems containing quinoline and 1,2,3-triazole systems 7a–h were obtained by reactions of ac...

One of the definitions of chemical biology is that it is a scientific discipline spanning the fields of chemistry, biology, and physics; it primarily involves the application of chemical techniques, tools, analyses, and often compounds (also known as chemical probes), which are produced through synthetic chemistry, in order to study and manipulate...

Nowadays, lipidomics plays a crucial role in the investigation of novel biomarkers of various diseases. Its implementation into the field of clinical analysis led to the identification of specific lipids and/or significant changes in their plasma levels in patients suffering from cancer, Alzheimer’s disease, sepsis, and many other diseases and path...

The search for the ideal metallic material for an implant is still a difficult challenge for scientists due to the phenomenon of corrosion and the consequent disruption of the implant structure. Prevention is the application of coatings that protect the implant, activate the tissues for faster regeneration, and also prevent inflammation through ant...

Many biologically active metabolites of the essential amino acid L-tryptophan (Trp) are associated with different neurodegenerative diseases and neurological disorders. Precise and reliable methods for their determination are needed. Variability in their physicochemical properties makes the analytical process challenging. In this case, chemical mod...

Targeted therapy represents a real opportunity to improve the health and lives of patients. Developments in this field are confirmed by the fact that the global market for drug carriers was worth nearly $40 million in 2022. For this reason, materials engineering and the development of new drug carrier compositions for targeted therapy has become a...

A series of nine 2,3-disubstituted-quinazolin-4(3H)-one derived Schiff bases and their three Cu(II) complexes was prepared and tested for their antimicrobial activities against reference strains Staphylococcus aureus ATCC 29213 and Enterococcus faecalis ATCC 29212 and resistant clinical isolates of methicillin-resistant S. aureus (MRSA) and vancomy...

Coating materials offers an intriguing solution for imparting inert implants with additional bioactive characteristics without changing underlying parameters such as mechanical strength. Metallic implants like endoprostheses or polymeric implants can be coated with a thin layer of bioactive film capable of stimulating bone-forming cells to prolifer...

Lipids represent a large group of biomolecules that are responsible for various functions in organisms. Diseases such as diabetes, chronic inflammation, neurological disorders, or neurodegenerative and cardiovascular diseases can be caused by lipid imbalance. Due to the different stereochemical properties and composition of fatty acyl groups of mol...

In an increasingly aging society, there is a growing demand for the development of technology related to tissue regeneration. It involves the development of the appropriate biomaterials whose properties will allow the desired biological response to be obtained. Bioactivity is strongly affected by the proper selection of active ingredients. The aim...

Optical rotation (OR), the most frequently used chiroptical method, is used for the characterization of newly synthesized or isolated compounds. Computational predictions of OR are, however, mainly used for the determination of the absolute configurations of chiral compounds, but they may also be used for the verification of conformational analysis...

Fungi are undoubtedly one of the most widespread groups of organisms on Earth. In addition to their multiple uses in various areas of human activities, fungi produce numerous volatile organic compounds (VOCs) based on hydrocarbons, alcohols, phenols, amines, carbonyl and carboxyl derivatives and heterocycles. These VOCs are able to affect both the...

As a result of the runoff losses of agrochemicals that have been used in excessive amounts over the last few decades from agricultural soils, the levels of these harmful chemicals have also increased in the aquatic ecosystem, where adverse impact on non-target organisms has been observed. The advantage of using nanoagrochemicals compared to convent...

In recent years, significant developments have taken place in scientific fields such as tissue and materials engineering, which allow for the development of new, intelligent biomaterials. An example of such biomaterials is drug delivery systems that release the active substance directly at the site where the therapeutic effect is required. In this...

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...

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...

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...

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...

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...

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...

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...

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...

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...

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...

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-...

Although it may not seem like it, chemical biology has existed for a long time from today’s perspective [...]

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...

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...

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...

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...

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...

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...

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...

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...

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...

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...

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....

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...

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...

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...

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...

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...

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...

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...

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...

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...

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...

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,...

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...

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...

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...

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...

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...

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...

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...

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...

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...

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...

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...

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...

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...

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...

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...

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...

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...

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...

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...

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...

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-...