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Derivatives of pyrazine as potential antituberculotics
Osička, Zdeněk ; Doležal, Martin (advisor) ; Kučerová, Marta (referee)
Mgr. Zdeněk Osička: Pyrazine Derivatives as potential antituberculous drugs I have focused on the synthesis of compounds from the class amides of substituted pyrazinoic acid in my Pharmacy Doctor Thesis. Series of compounds were prepared by the reaction of pyrazinoic acid chloride with corresponding amines. Synthesis underwent in two steps. Final compounds were characterized by the melting point, TLC, elementary analysis, 1H a 13C NMR and IR. All compounds were liable in vitro testing on their biological activity - antimycobacterial, antifungal and antibacterial. In the group of antituberculosis testing the activity grew up from the least to the most lipophility compound.
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Synthesis and comparison of activity of potential reactivators of acetylcholinesterase inhibited by cyclosarine
Lipka, Lukáš ; Doležal, Martin (advisor) ; Kučerová, Marta (referee)
SYNTHESIS OF POTENCIAL QUATERNARY ACETYLCHOLINESTERASE REACTIVATORS AND EVALUATION OF THEIR POTENCY TO REACTIVATE CYCLOSARIN-INHIBITED AChE Mgr. Lukáš Lipka Department of pharmaceutical chemistry and drug control, Charles University in Prague, Faculty of Pharmacy in Hradec Králové, Heyrovského 1203, 500 05 Hradec Králové, Czech Republic Abstract of the rigorous thesis: Nine potential AChE reactivators were synthesized. Their potency to reactivate AChE inhibited by cyclosarin nerve agent was tested in vitro. According to the obtained results, 1,4- bis(2-hydroxyiminomethylpyridinium)butane dibromide seems to be most potent AChE reactivator. The reactivation potency of these compounds depends on structural factors such as presence of quaternary nitrogens, lenght of the linking chain between both pyridinium rings, and position of the oxime moiety at the pyridinium ring. The independence of potency of reactivator trimedoxim at the kind of anion present in his molecule was validate.
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Azaphthalocyanines as new structural group of fluorescence quencher.
Kopecký, Kamil ; Doležal, Martin (advisor) ; Lang, Kamil (referee) ; Pour, Milan (referee)
1 SUMMARY This dissertation thesis deals with searching of structurally new non-fluorescent quenchers of fluorescence, which may be used for preparation of molecular probes. These potential quenchers are derived from asymmetrically substituted alkylaminoderivatives of tetrapyrazinoporphyrazines - azaphthalocyanines. As the part of this work is preparation of precursors - 5,6-disubstituted pyrazine-2,3-dicarbonitriles. They are starting material for the preparation of final substances - tetrapyrazinoporphyrazines bearing different functional moieties. In total were prepared: 14 intermediates (3 of them have been described in our department) 13 final tetrapyrazinoporphyrazines (1 of them has been described in our department) 1 modified solid phase suitable for synthesis of marked oligonucleotides 2 by-products 23 undescribed compounds were prepared. Synthesis of 4 substances was not successful. Final products were tested for their singlet oxygen quantum yields, stability in solutions used for synthesis of oligonucleotides and subsequently ability of quenching of commercially available fluorofor Cy5® . This ability was compared with commercially available quencher Black Hole Quencher-2® . As a part of this work is confirmation of distribution of congeners arising during the statistical tetramerization of...
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Pregnancy and profession of a nurse
Rusnáková, Marcela ; Tomová, Šárka (advisor) ; Doležal, Martin (referee)
The thesis discusses tbe attitude of nurses and women, without medical education, to pregnancy and childbirths on tbe bases of questionnaires which were distributed to women who were already pregnant or women who are nowadays pregnant. The thesis is divided into two parts - the theoretical and tbe empirical one. Tbe theoretical part re1ates to pregnancy and its physiological process, eating during pregnancy, prenamI care and possibilities of giving birth in the Czech Republic. Trus part is also about the nurse profession and above aH it is about risks taking at work. Tbe second empirical part relates to analysis of questionnaires results. The fmal assessment of the thesis includes appendices. Powered by TCPDF (www.tcpdf.org)
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Derivatives of pyrazine as potential antituberculars (preparation and study of biological properties)
Janďourek, Ondřej ; Doležal, Martin (advisor) ; Farsa, Oldřich (referee) ; Musílek, Kamil (referee)
Charles University, Faculty of Pharmacy in Hradec Králové Department of Pharmaceutical chemistry and Pharmaceutical analysis Candidate Mgr. Ondřej Janďourek Supervisor Prof. PharmDr. Martin Doležal, Ph.D. Consultant PharmDr. Jan Zitko, Ph.D. Title of Doctoral Thesis Derivatives of pyrazine as potential antituberculars (preparation and study of biological properties) This work is focused on pyrazine derivatives with the structural relationship to pyrazinamide (PZA) and with the potential antitubercular effect. In the introduction, there are summarized theoretical findings about tuberculosis (TBC), its epidemiology and primarily the development of resistance to current pharmacotherapy. Brief overview of known antituberculars, novel compounds and auspicious molecules in clinical trials is outlined. PZA, which is counted among the first line antitubercular agents, is widely described due to its cardinal role in this thesis. PZA possible mechanisms of action are described together with its pharmacological profile. Finally, brief summary of already prepared derivatives of PZA is stated. Practical part of this thesis is focused on synthesis of three starting compounds (5-chloro-6-methylpyrazine-2,3-dicarbonitrile; 3-chloropyrazine-2-carboxamide; N-benzyl-3-chloropyrazine-2-carboxamide) that were...
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