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Studying the distribution of substituents in derivatives based on hyaluronane
Sedláček, Jakub ; Šatínský, Dalibor (advisor) ; Zimčík, Petr (referee) ; Chmelař, Josef (referee)
Charles University, Faculty of Pharmacy in Hradec Králové Department of Analytical Chemistry Candidate Ing. Jakub Sedláček Supervisor doc. RNDr. Dalibor Šatínský, Ph.D. Title of Doctoral Thesis Studying the distribution of substituents in derivatives based on hyaluronan Derivatives based on hyaluronan have found applications in various areas of medicine. Prepared derivatives are commonly characterized by their molar mass and their degree of substitution, however, such parameters are unable to distinguish among derivatives with different distributions of substituents along the chain, which may exhibit different macroscopic properties. For this reason, methods to determine the distribution of substituents along the chain are needed. The presented thesis deals with the determination of distribution of amino groups in deacetylated hyaluronan. The theoretical part starts with a description of hyaluronan structure and of its derivatives. Next, the application, the preparation, and the characterization of deacetylated hyaluronan are discussed, focusing particularly on its depolymerisation into oligosaccharides using deaminative cleavage or enzymes that degrade hyaluronan. Finally, examples of liquid chromatographic methods used to analyse hyaluronan oligosaccharide are presented. The experimental part...
Derivatives combining the fragment of pyrazinamide and 4-aminosalicylic acid as antimycobacterial compounds
Šlechta, Petr ; Zitko, Jan (advisor) ; Zimčík, Petr (referee)
Charles University Faculty of Pharmacy in Hradec Králové Department of Pharmaceutical chemistry and Pharmaceutical analysis Author: Petr Šlechta Supervisor: doc. PharmDr. Jan Zitko, Ph.D. Consultant: MSc. Ghada Basem Bouz, Ph.D. Title of diploma thesis: Derivatives combining the fragment of pyrazinamide and 4-aminosalicylic acid as antimycobacterial compounds According to WHO, tuberculosis (TB) is the leading cause of death from a single infectious organism worldwide and the number of cases with drug resistant TB is still increasing, creating the need for new antituberculotics. Therefore, we report design, synthesis and antimicrobial evaluation of a series of hybrid compounds combining different pyrazinamide derivates and p- aminosalicylic acid as potential antituberculotic agents. The compounds were prepared by mixing different pyrazinecarboxylic acids, after activation by 1,1'-carbonyldiimidazole, with p- aminosalicylic acid in dimethylsulfoxide as a solvent. Obtained compounds were in vitro tested for their antimycobacterial activity against M. tuberculosis H37Rv, M. tuberculosis H37Ra and four other mycobacterial strains. Prepared compounds were also in vitro screened for antibacterial, antifungal, and cytotoxic (HepG2) activity. Most compounds showed antimycobacterial activity in range of...
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...
Synthesis and delivery of novel fluorescently-labelled nucleotides and their nucleic acids for bio-analytical applications
Güixens Gallardo, Pedro ; Hocek, Michal (advisor) ; Zimčík, Petr (referee) ; Klán, Petr (referee)
1 Abstract The goals of the thesis were to synthesise novel fluorescently labelled nucleotides and the corresponding nucleic acids for bio-analytical applications as well as their delivery into cells. The thesis also aimed at the development of an effective method to inhibit non-templated incorporation of nucleotides. The problematic non-templated enzymatic incorporation of nucleotides is addressed by using several commercially available 5'-modified-oligonucleotides. The oligonucleotides (ONs) that we tested bore ortho twisted intercalating nucleic acid (oTINA), a trityl group, or biotin at the 5'-end. The modified ONs were used as templates in the enzymatic primer extension (PEX) experiments in the presence of either modified nucleotides or only natural deoxynucleoside triphosphates (dNTPs). The oTINA templates underwent PEX reaction using natural dNTPs and different DNA polymerases of the A or B family. In parallel, two types of fluorescent nucleoside derivatives were independently designed and synthesised. Firstly, we envisaged new fluorescent nucleotide tags containing the hexamethylated BODIPY moiety as a bright fluorescent label. Conversely, we focused on the improvement of fluorescent nucleotide probes sensitive to the viscosity or polarity. The fluorescently labelled methylated BODIPY nucleotides...
Synthesis of anionic phthalocyanines as potential photodynamic active photosensitizers
Kollár, Jan ; Zimčík, Petr (advisor) ; Mosinger, Jiří (referee) ; Zitko, Jan (referee)
Charles University, Faculty of Pharmacy in Hradec Kralove Department: Department of Pharmaceutical Chemistry and Pharmaceutical Analysis Author: Mgr. Jan Kollar Supervisor: prof. PharmDr. Petr Zimcik, Ph.D. Advisor: doc. PharmDr. Veronika Novakova, Ph.D. Doctoral Thesis: Synthesis of anionic phthalocyanines as potential photodynamic active photosensitizers Phthalocyanines (Pcs) and their aza-analogues (e.g. tetrapyrazinoporphyrazines, TPyzPzs) represent a promising group of organic dyes with interesting photophysical properties (strong absorption in area 650-750 nm, strong singlet oxygen production) highly suitable for the use in photodynamic therapy (PDT) of cancer. However, they have also some drawbacks lowering their potential use in PDT (low solubility in water, strong tendency to aggregate). The topic of my dissertation thesis closely follows the topic of my diploma thesis, during which TPyzPz with sixteen carboxylate groups in rigid arrangement was prepared and in which we have disclosed strong negative effect of low pH and serum proteins on photodynamic activity. In the first part of this thesis I prepared new zinc TPyzPz with eight sulfonate groups on periphery, which was characterised by good solubility in water. Sulfonates were chosen as stronger acids than carboxylic groups, so they were...
Synthesis of anionic phthalocyanines as potential photodynamic active photosensitizers
Kollár, Jan ; Zimčík, Petr (advisor) ; Mosinger, Jiří (referee) ; Zitko, Jan (referee)
Charles University, Faculty of Pharmacy in Hradec Kralove Department: Department of Pharmaceutical Chemistry and Pharmaceutical Analysis Author: Mgr. Jan Kollar Supervisor: prof. PharmDr. Petr Zimcik, Ph.D. Advisor: doc. PharmDr. Veronika Novakova, Ph.D. Doctoral Thesis: Synthesis of anionic phthalocyanines as potential photodynamic active photosensitizers Phthalocyanines (Pcs) and their aza-analogues (e.g. tetrapyrazinoporphyrazines, TPyzPzs) represent a promising group of organic dyes with interesting photophysical properties (strong absorption in area 650-750 nm, strong singlet oxygen production) highly suitable for the use in photodynamic therapy (PDT) of cancer. However, they have also some drawbacks lowering their potential use in PDT (low solubility in water, strong tendency to aggregate). The topic of my dissertation thesis closely follows the topic of my diploma thesis, during which TPyzPz with sixteen carboxylate groups in rigid arrangement was prepared and in which we have disclosed strong negative effect of low pH and serum proteins on photodynamic activity. In the first part of this thesis I prepared new zinc TPyzPz with eight sulfonate groups on periphery, which was characterised by good solubility in water. Sulfonates were chosen as stronger acids than carboxylic groups, so they were...
Synthesis and investigation of aminophthalocyanines II.
Mocák, Ivan ; Zimčík, Petr (advisor) ; Zitko, Jan (referee)
Charles University, Faculty of Pharmacy in Hradec Králové Department of Pharmaceutical Chemistry and Pharmaceutical Analysis Candidate: Ivan Mocák Supervisor: prof. PharmDr. Petr Zimčík, Ph.D. Title of diploma thesis: Synthesis and investigation of aminophthalocyanines II. Azaphthalocyanines (AzaPc) are nitrogen analogues of phthalocyanines (Pc) where benzene rings are replaced for pyrazine, pyridine or pyridazine respectively. AzaPc are characterized by broad spectrum of characteristic photophysical and photochemical properties that are responsible for their use in many areas, e.g. as industrial dyes, as photosensitizers in photodynamic therapy or as fluorescent sensors. In recent years, importance of dialkylamino substituted AzaPc has been rising in area of fluorescence quenching. Their broad absorption spectrum makes them suitable candidates to become universal quenchers. Process responsible for their quenching ability is called intramolecular charge transfer (ICT) from peripheral dialkylamino groups. These groups are also responsible for formation of unique supramolecular arrangement - J-dimers. The influence of bulky dialkylamino substituents on formation of J-dimers, which occurrence is rarer than the other possible form - H-dimers, is studied in this work. Results also describe how ICT is...
Synthesis of novel 5,6-disubstituted derivatives of uracil as potential drugs
Vu, Lien Phuong ; Kučerová, Marta (advisor) ; Zimčík, Petr (referee)
Charles University Faculty of Pharmacy in Hradec Králové Department of Pharmaceutical Chemistry and Pharmaceutical Analysis Candidate: Vu Lien Phuong Supervisors: PharmDr. Marta Kučerová, Ph.D. Tanja Bruun, M.Sc. (Pharm.) Prof. Jari Yli-Kauhaluoma Title of diploma thesis: Synthesis of novel 5,6-disubstituted derivatives of uracil as potential drugs In this thesis, uracil was used as the core structure given its many biological activities that were reported such as antitumor, antiviral, antibiotic, hypoglycemic, diuretic and many others. The work was focused on the preparation of new 5,6- disubstituted uracil derivatives as potential biologically active agents. 2,4,6-Trichloropyrimidine was used for the preparation of 6-chlorouracil that was condensed with phenols or anilines to give the respective 6-phenoxyuracils and 6- phenylaminouracils. These intermediates were then modified in position 5 to give the final products. For this very challenging last step, various alkylating and acylating agents were used, e.g. Vilsmeier reagent, alkylchlorides, chloroacetyl chloride, ethyl chlorooxoacetate and ethyl bromoacetate. In the end, ethyl bromoacetate gave the most promising results affording four novel 5,6-disubstituted uracil derivatives. During the experimental work it was found that pH of water used...
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...
The electrochemical reduction of the nitro group in a flow reactor
Jankových, Miroslav ; Kučera, Radim (advisor) ; Zimčík, Petr (referee)
Charles University Faculty of Pharmacy in Hradec Králové Department of Pharmaceutical chemistry and Pharmaceutical analysis Student: Miroslav Jankových Supervisor: doc. PharmDr. Radim Kučera, PhD. Consultant: PharmDr. Tomáš Holas, PhD. Title of diploma thesis: The electrochemical reduction of the nitro group in a flow reactor The aim of this diploma thesis is to study the electrochemical reduction within the flow reactor. The combination of these two methods provides enviromentaly-friendly and interesting method for the manufacturing of active pharmaceutical ingredients. Our object was to find out if the reaction really goes on. After that our goals were to optimize the reaction parameters. We executed some of the experiments to understand the parameters such as: flow rate, voltage, electric current, electrolyte. These parameters we combined to see their effect on the reaction results. The outcome of the thesis is mainly basic information about impact of parameters mentioned above. From the series of experiments the best parameters are flow rate 0,1 ml.min- 1 , voltage 0,8 - 2,0 V, electric current 100 - 150 mA, electrolyte NH4Cl, reaching conversion up to 96%.

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