National Repository of Grey Literature 16 records found  1 - 10next  jump to record: Search took 0.00 seconds. 
Design, synthesis and evaluation of heterocyclic compounds with potential antimicrobial activity I
Brányik, Michal ; Zitko, Jan (advisor) ; Demuth, Jiří (referee)
Charles University, Faculty of Pharmacy in Hradec Králové Department of Pharmaceutical Chemistry and Pharmaceutical Analysis Title of the thesis: Design, synthesis and evaluation of heterocyclic compounds with potential antimicrobial activity I Author: Michal Brányik Supervisor: doc. PharmDr. Jan Zitko, Ph.D. Consultant: PharmDr. Martin Juhás, Ph.D. Antimicrobial resistance is an ever-growing problem that occurs worldwide. Many bacterial strains develop the ability to resist the otherwise efficient substances, thus posing a serious threat for the future. Mycobacterium tuberculosis (Mtb), the source of tuberculosis, is no exception. Given that it is the leading cause of death due to a single pathogen, many efforts have been put into finding new active compounds. The substances synthesized as a part of this thesis are based on previously prepared substances with potential antimicrobial activity. The basic structure consists of 2-aminooxazole or 2-aminothiazole and substituted pyridine or pyrazine carboxamides. The structures were confirmed by the 1 H and 13 C NMR spectra, IR spectra and mass spectrometry. All the substances were tested for in vitro activity against eight bacterial strains (four gram-positive and four gram-negative) as well as eight fungal strains (four yeast and four fungi). We also...
Preparation of conjugates oligonucleotide probes with functional molecules.
Grossová, Petra ; Miletín, Miroslav (advisor) ; Demuth, Jiří (referee)
Charles University, Faculty of Pharmacy in Hradec Králové Department of Pharmaceutical Chemistry and Pharmaceutical Analysis Supervisor: doc. PharmDr. Miroslav Miletín, Ph.D. Consultant: Mgr. Michaela Beranová Student: Petra Grossová Title of Thesis: Preparation of conjugates oligonucleotide probes with functional molecules The aim of this thesis was to find the optimal conditions for conjugation of an oligonucleotide to a fluorescent dye by solid-phase click chemistry. The traditional fluorescent dye Cyanine5 was chosen as the labelling molecule. The effect of the concentration of fluorescent dye, the position of the labelling, the type of solid phase and the reaction time were examined. The deprotection conditions were optimized. Two series of reactions followed by deprotection and purification were performed. The efficiency of the reaction was evaluated by comparing the peak areas under the curve of conjugated and unconjugated molecules in the chromatograms of the samples after analysis by HCPL with UV detection. Peak integration was performed in LabSolutions software. The reactions running on the polystyrene solid phase gave the highest yields, with labelling at any position of the chain. For labelling at the 5'-end of the chain, more than 90% efficiency was achieved using all tested solid...
Synthesis and study of supramolecular properties of azaphthalocyanines usable as sensors
Sikorová, Eliška ; Demuth, Jiří (advisor) ; Kučerová, Marta (referee)
Charles University, Faculty of Pharmacy in Hradec Králové Department Department of Pharmaceutical Chemistry and Pharmaceutical Analysis Candidate Eliška Sikorová Supervisor PharmDr. Jiří Demuth, Ph.D. Title of ThesisSynthesis and study of supramolecular properties of azaphthalocyanines usable as sensors Azaphthalocyanines are planar aromatic macrocycles that were derived from natural porphyrins. The basic skeleton consists of four isoindole units which are linked at positions 1 and 3 by azamethine bridges, resulting in an extensive system of conjugated double bonds that give these compounds unique optical and electrical properties. Azaphthalocyanines are widely used as industrial dyes, conductors, photosensitizers in photodynamic therapy, fluorescence quenchers or fluorescence sensors, etc. The compounds synthesized during this thesis can be used as an interesting type of sensors for sensing coordination analytes in solution. That is why this work deals with the study of the supramolecular properties of the synthesized compounds, in particular the ability to form J-dimer type aggregates, which are formed by coordination of the peripheral pyridyl nitrogen to the central zinc cation of the second azapthalocyanine. J-dimers resemble a "step-like" arrangement in contrast to the second type of...
Design, synthesis and evaluation of heterocyclic compounds with potential antimicrobial activity I
Brányik, Michal ; Zitko, Jan (advisor) ; Demuth, Jiří (referee)
Charles University, Faculty of Pharmacy in Hradec Králové Department of Pharmaceutical Chemistry and Pharmaceutical Analysis Title of the thesis: Design, synthesis and evaluation of heterocyclic compounds with potential antimicrobial activity I Author: Michal Brányik Supervisor: doc. PharmDr. Jan Zitko, Ph.D. Consultant: PharmDr. Martin Juhás, Ph.D. Antimicrobial resistance is an ever-growing problem that occurs worldwide. Many bacterial strains develop the ability to resist the otherwise efficient substances, thus posing a serious threat for the future. Mycobacterium tuberculosis (Mtb), the source of tuberculosis, is no exception. Given that it is the leading cause of death due to a single pathogen, many efforts have been put into finding new active compounds. The substances synthesized as a part of this thesis are based on previously prepared substances with potential antimicrobial activity. The basic structure consists of 2-aminooxazole or 2-aminothiazole and substituted pyridine or pyrazine carboxamides. The structures were confirmed by the 1 H and 13 C NMR spectra, IR spectra and mass spectrometry. All the substances were tested for in vitro activity against eight bacterial strains (four gram-positive and four gram-negative) as well as eight fungal strains (four yeast and four fungi). We also...
Synthesis and study of subphthalocyanines axially modified with an amino adamantyl
Danková, Eva ; Nováková, Veronika (advisor) ; Demuth, Jiří (referee)
Charles University, Faculty of Pharmacy in Hradec Králové Department Department of Pharmaceutical Chemistry and Pharmaceutical Analysis Candidate Eva Danková Supervisor doc. PharmDr. Veronika Nováková, Ph.D. Title of Thesis Synthesis and study of subphthalocyanines axially modified by amino adamanthyl Photodynamic therapy is a promising approach for cancer treatment that relies on the administration of a photosensitizer, followed by illumination of the tumor. The generated oxidative stress subsequently activates several mechanisms of cell death. One of the novel groups of photosensitizers are subphthalocyanines with a conical π surface, which renders them less prone to aggregation and offers the possibility to tune their properties through axial substitution (aside peripheral modification). Due to the lipofilicity of the macrocycle, it is necessary to increase its water solubility. This work focused on the possibility of forming supramolecular host-guest complexes with hydrophilic macrocycles in order to increase the hydrophilicity of a subphthalocyanine. In particular, cucurbituril-7 (CB[7]) was chosen since it forms one of the most stable supramolecular interactions in water with 1-aminoadamantane, which was therefore proposed as the axial substituent on subphthalocyanine core. Synthesis of the...
Design, synthesis and evaluation of pyridine derivatives as potential antimicrobial compounds
Bachtíková, Andrea ; Zitko, Jan (advisor) ; Demuth, Jiří (referee)
Charles University, Faculty of Pharmacy in Hradec Králové Department of Pharmaceutical Chemistry and Pharmaceutical Analysis Thesis title: Design, synthesis and evaluation of pyridine derivatives as potential antimicrobial compounds Author: Andrea Bachtíková Thesis supervisor: doc. PharmDr. Jan Zitko, Ph.D. Consultant: PharmDr. Martin Juhás Tuberculosis is a global problem even today. It is the second most common cause of death from infectious diseases according to the WHO and resistance to common antituberculosis drugs, which have been used in therapy for decades, increases. These facts are the main reasons why research into new potential drugs is needed. This thesis presents design, synthesis and evaluation of antimicrobial properties of a series of substituted N-oxazolyl and N-thiazolyl carboxamides of different pyridinecarboxylic acids. Final compounds were characterized by 1 H and 13 C-NMR spectroscopy, IR spectra, melting point and HRMS (High resolution mass spectrometry). Obtained compounds were tested for in vitro activity against M. tuberculosis H37Rv, M. tuberculosis H37Ra and four other clinically less important mycobacterial strains. In addition, compounds were tested for antibacterial activity against four G+ and four G- bacterial strains, antifungal activity against yeasts and fungi,...
Synthesis and study of subphthalocyanines axially modified with an amino adamantyl
Danková, Eva ; Nováková, Veronika (advisor) ; Demuth, Jiří (referee)
Charles University, Faculty of Pharmacy in Hradec Králové Department Department of Pharmaceutical Chemistry and Pharmaceutical Analysis Candidate Eva Danková Supervisor doc. PharmDr. Veronika Nováková, Ph.D. Title of Thesis Synthesis and study of subphthalocyanines axially modified by amino adamanthyl Photodynamic therapy is a promising approach for cancer treatment that relies on the administration of a photosensitizer, followed by illumination of the tumor. The generated oxidative stress subsequently activates several mechanisms of cell death. One of the novel groups of photosensitizers are subphthalocyanines with a conical π surface, which renders them less prone to aggregation and offers the possibility to tune their properties through axial substitution (aside peripheral modification). Due to the lipofilicity of the macrocycle, it is necessary to increase its water solubility. This work focused on the possibility of forming supramolecular host-guest complexes with hydrophilic macrocycles in order to increase the hydrophilicity of a subphthalocyanine. In particular, cucurbituril-7 (CB[7]) was chosen since it forms one of the most stable supramolecular interactions in water with 1-aminoadamantane, which was therefore proposed as the axial substituent on subphthalocyanine core. Synthesis of the...
Synthesis of isoprenoid naringenin derivatives
Kernal, Jakub ; Zimčík, Petr (advisor) ; Demuth, Jiří (referee)
5 Abstract Charles University, Faculty of Pharmacy in Hradec Králové Department Department of Pharmaceutical Chemistry and Pharmaceutical Analysis Candidate Jakub Kernal Supervisor prof. PharmDr. Consultant Hubert Chapuis, Ph.D. Title of Thesis Synthesis of Isoprenoid Naringenin Derivatives Naringenin as a member of flavanone subclass of flavonoids and its derivatives have been subjects of intensive study for their antibacterial, antifungal, and antineoplastic properties. Recent development in current methods of synthetic chemistry allows us to satisfy the increasing demand for these molecules by providing an alternative source of these naturally occurring substances in the means of chemical synthesis. The aim of this work was synthesis and characterization of naringenin derivatives with increased lipophilic profile which will serve in future research as potential cytotoxic agents. Two major approaches have been developed in the process of obtaining lipophilic derivatives of naringenin (Fig. 2) where the lipophilic moiety consists of terpene or terpenoid part, which is believed to increase the uptake of the desired product by cells. In the first approach, we focused on the modification of the B phenolic ring by esterification of the hydroxyl group on the 4 carbon or on the modification of both A and B...
Study of azaphthalocyanines as fluorescence quenchers in oligodeoxynucleotide probes
Demuth, Jiří ; Nováková, Veronika (advisor) ; Hocek, Michal (referee) ; Vávrová, Kateřina (referee)
Charles University, Faculty of Pharmacy in Hradec Kralove Department: Department of Pharmaceutical Chemistry and Pharmaceutical Analysis Author: Mgr. Jiří Demuth Supervisor: doc. PharmDr. Veronika Nováková, Ph.D. Consultant: prof. PharmDr. Petr Zimčík, Ph.D. Doctoral Thesis: Study of azaphthalocyanines suitable for quenching of fluorescence in oligodeoxynucleotide probes Phthalocyanines (Pcs) and azaphthalocyanines (AzaPcs) are planar macrocyclic compounds. These synthetic compounds are derived from naturally occurring dyes - porphyrins. Pcs and AzaPcs have very interesting photophysical properties due to their extensive 18 -electron conjugated system. They are used in electrotechnics, material industry or in medicinal applications. Octaalkylamino substituted tetrapyrazinoporphyrazines (TPyzPzs), which belong to AzaPc family, can quench fluorescence of other molecules due to the ultrafast intramolecular charge transfer. This thesis studies this quenching ability of TPyzPzs with the aim to develop efficient fluorescence probes. Such probes could find application in a variety of experiments across scientific disciplines i.e. - biochemistry, forensic or genetic analysis. Synthetic part of dissertation thesis is a continuation of previous investigation of TPyzPzs in our research group. It describes...
Study of azaphthalocyanines as fluorescence quenchers in oligodeoxynucleotide probes
Demuth, Jiří ; Nováková, Veronika (advisor) ; Hocek, Michal (referee) ; Vávrová, Kateřina (referee)
Charles University, Faculty of Pharmacy in Hradec Kralove Department: Department of Pharmaceutical Chemistry and Pharmaceutical Analysis Author: Mgr. Jiří Demuth Supervisor: doc. PharmDr. Veronika Nováková, Ph.D. Consultant: prof. PharmDr. Petr Zimčík, Ph.D. Doctoral Thesis: Study of azaphthalocyanines suitable for quenching of fluorescence in oligodeoxynucleotide probes Phthalocyanines (Pcs) and azaphthalocyanines (AzaPcs) are planar macrocyclic compounds. These synthetic compounds are derived from naturally occurring dyes - porphyrins. Pcs and AzaPcs have very interesting photophysical properties due to their extensive 18 -electron conjugated system. They are used in electrotechnics, material industry or in medicinal applications. Octaalkylamino substituted tetrapyrazinoporphyrazines (TPyzPzs), which belong to AzaPc family, can quench fluorescence of other molecules due to the ultrafast intramolecular charge transfer. This thesis studies this quenching ability of TPyzPzs with the aim to develop efficient fluorescence probes. Such probes could find application in a variety of experiments across scientific disciplines i.e. - biochemistry, forensic or genetic analysis. Synthetic part of dissertation thesis is a continuation of previous investigation of TPyzPzs in our research group. It describes...

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