National Repository of Grey Literature 4 records found  Search took 0.01 seconds. 
Ability of copper chelators to interact with iron and zinc
Hanuščinová, Lucia ; Mladěnka, Přemysl (advisor) ; Čonka, Patrik (referee)
Charles University Faculty of Pharmacy in Hradec Králové Department of Pharmacology and Toxicology Student: Lucia Hanuščinová Supervisor: Assoc. Prof. Přemysl Mladěnka, PharmDr., PhD. Title of diploma thesis: Ability of copper chelators to interact with iron and zinc Copper plays in the human organism a role of an element with indispensable significance, whose biological influence and effects depend on its quantity. With elevated concentrations in the human body, copper becomes toxic, resulting in pathological conditions. The most well-known diseases is the Wilson's disease, whose treatment consists of oral administration of chelators, i.e. chemical compounds, which are capable of binding copper ions in various proportions and eliminating them from the organism. Chelation therapy is currently the first choice after confirmation of the diagnosis. Chelation toxicity results from several factors, e.g. inhibition of copper dependent enzymes or low selectivity to metals. And precisely the selectivity of chelators is being discussed in this diploma thesis. An ideal chelator should not interact with any of the other physiological ions, that are necessary for the proper functioning of the organism. Five of the most frequently therapeutically or experimentally used substances /trientine, D-penicillamine,...
Ability of copper chelators to interact with iron and zinc
Hanuščinová, Lucia ; Mladěnka, Přemysl (advisor) ; Čonka, Patrik (referee)
Charles University Faculty of Pharmacy in Hradec Králové Department of Pharmacology and Toxicology Student: Lucia Hanuščinová Supervisor: Assoc. Prof. Přemysl Mladěnka, PharmDr., PhD. Title of diploma thesis: Ability of copper chelators to interact with iron and zinc Copper plays in the human organism a role of an element with indispensable significance, whose biological influence and effects depend on its quantity. With elevated concentrations in the human body, copper becomes toxic, resulting in pathological conditions. The most well-known diseases is the Wilson's disease, whose treatment consists of oral administration of chelators, i.e. chemical compounds, which are capable of binding copper ions in various proportions and eliminating them from the organism. Chelation therapy is currently the first choice after confirmation of the diagnosis. Chelation toxicity results from several factors, e.g. inhibition of copper dependent enzymes or low selectivity to metals. And precisely the selectivity of chelators is being discussed in this diploma thesis. An ideal chelator should not interact with any of the other physiological ions, that are necessary for the proper functioning of the organism. Five of the most frequently therapeutically or experimentally used substances /trientine, D-penicillamine,...
Synthesis of tetrazoles as anticuberculotics
Vicherek, Petr ; Čonka, Patrik (advisor) ; Klimešová, Věra (referee)
Charles University in Prague Faculty of Pharmacy in Hradec Králové Department of Inorganic and Organic Chemistry Candidate: Petr Vicherek Supervisor: RNDr. Patrik Čonka, Ph.D. Title of diploma thesis: Synthesis of tetrazoles as antituberculotics Although significant progress in therapy of tuberculosis has been made since effective drugs were discovered in the second half of the 20th century, it is still widespread and refractory curable disease. The situation is complicated with growing appearance of resistant strains and for that reason it is necessary to search for new potential antituberculotics. The aim of this work was to continue with synthesis of antimycobacterial-efficient structures based on tetrazole. Firstly, we synthesised derivates of 1-aryl-5-[(3,5-dinitrobenzyl)sulfanyl]-1H-tetrazole by the method of Williamson's synthesis, when the reaction of 1-aryl-1H-tetrazol-5-thiol with 3,5-dinitrobenzylchloride was performed. Conditions of the reactions were further optimalised. We prepared by the same way derivates of 1-fenyl-5-[(3,4,5- trimethoxybenzyl)sulfanyl]-1H-tetrazole afterwards, as analogues of previous tetrazoles missing the electron withdrawing 3,5-dinitrosubstitution. Furthermore, we concentrated on synthesis of substituted 1,5-diphenyl-1H-tetrazoles. Substituted...
Synthesis of 4-nitrosalicylanilide derivatives with potential antibacterial activity (Syntéza 4-nitrosalicylanilidových derivátů s potenciální antibakteriální aktivitou)
Karagianni, Styliani ; Vinšová, Jarmila (advisor) ; Čonka, Patrik (referee)
Karagianni Styliani Synthesis of 4-nitrosalicylanilide derivatives with potential antibacterial activity Diploma thesis Charles University in Prague, Faculty of Pharmacy in Hradec Kralove Pharmacy Background: The point of this diploma work was the synthesis of 4- nitrosalicylanilide derivatives, as a possible antibacterial agents against Mycobacterium tuberculosis. Methods: All reactions were monitored, and the purity of products was verified by TLC in which the plates were coated with silica gel 60 F254. They were also visualized using UV irradiation, while the column chromatography, was performed using silica gel 60. The melting points of products were determined on a Melting Point apparatus and Büchi are uncorrected, IR spectra were recorded using ATR technique and the NMR spectra were measured in DMSO-d6 or CDCl3. Results: The reactions between the starting compounds were successfully proceeded under the microwave reactor and the presence of chlorobenzene, trimethylamine and phosphorus trichloride. Conclusion: Unfortunately some of the final products of these experiments were probably triethylamine salts of salicylanilides that was determined on NMR spectra.

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