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Development of a bioanalytical method for the determination of novel drug candidates derived from thiosemicarbazone in a biological material
Suprunová, Vlasta ; Stariat, Ján (advisor) ; Kučera, Radim (referee)
Nowadays, high-performance liquid chromatography is widely used analytical method for separation and quantification of drugs in biological material due to its high sensitivity and selectivity. HPLC is suitable for quantitative as well as qualitative analysis. 2-benzoylpyridine-4-ethyl-3-thiosemicarbazone (Bp4eT) is a potential drug from the group of thiosemicarbazones, which are currently intensively studied and developed as anticancer agents. Their specific mechanism of action, based on chelation of iron, might overcome resistance to standard chemotherapy. The aim of this study was to develop and assess essential validation parameters of an HPLC-MS/MS method for determination of Bp4eT and its main phase I metabolites in rat plasma and to utilise the method for the analysis of samples from a pilot pharmacokinetic study in rats. The separation of Bp4eT and its metabolites was achieved on chromatographic column Discovery HSC18 (75 x 4.6 mm, 3 µm) protected by the same type of guard column using the mobile phase consisting of ammonium formate and acetonitrile in ratio 40:60 (v/v). The isocratic elution and the flow rate of 0.4 ml/min were utilised. Mass spectrometer was chosen as a detector and the quantification was performed in selected reaction monitoring mode. Plasma samples were treated using the...
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METABOLISM AND EFFECTS OF NEW ANTHELMINTIC DRUG IN HELMINTHS AND ITS HOSTS
Stuchlíková, Lucie ; Skálová, Lenka (advisor) ; Kučera, Radim (referee) ; Machala, Miroslav (referee)
Charles University in Prague Faculty of Pharmacy in Hradec Králové Department of Biochemical Sciences Candidate Mgr. Lucie STUCHLÍKOVÁ Supervisor prof. RNDr. Lenka SKÁLOVÁ, Ph.D. Title of Doctoral Thesis METABOLISM AND EFFECTS OF NEW ANTHELMINTIC DRUG IN HELMINTHS AND ITS HOSTS Diseases caused by helminths, called helminthoses, are one of the most serious problems in veterinary and human medicine. These diseases are treated by anthelmintics but their effectiveness is often not sufficient due to resistance of helminths against common anthelmintics. The global anthelmintic resistance encouraged the developing of new drugs with a different mode of action. Monepantel (MOP) belongs to a new class of anthelmintic drugs known as amino- acetonitrile derivatives (AADs) that act on the nicotinic acetylcholine receptors. In 2011, MOP was approved for the treatment of gastrointestinal diseases caused by nematodes in the veterinary practice in the Czech Republic. It is produced commercially under the trade name Zolvix® (Novartis AG). The aim of this doctoral thesis was to study metabolism and effects of MOP and other AADs in order to contribute to the global research in this field. For this purpose, adults nematodes Haemonchus contortus (the sensitive strain ISE and the resistant strain WR) and its hosts Ovis...
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Chiral separation of boron cluster compounds II.
Zámyslická, Yvette ; Kučera, Radim (advisor) ; Kastner, Petr (referee)
Charles University Faculty of Pharmacy in Hradec Králové Department: Department of Pharmaceutical Chemistry and Pharmaceutical Analysis Candidate: Yvette Zámyslická Supervisor: doc. PharmDr. Radim Kučera, Ph.D. Consultant: RNDr. Ondřej Horáček, Ph.D. Title od Thesis: Chiral separations of borane cluster compounds II. This diploma thesis focuses on screening and optimisation of chiral separations of borane cluster compounds. Approximately more than half of the currently used medications are chiral compounds whose isomers can differ in biological activity. Borane cluster compounds, some of which are chiral, represent a significant substance category due to their chiral aspects which offer new possibilities in synthesis and modification of drug structures. The aim of this diploma thesis is to propose an optimised approach for the analysis of borane cluster compounds and achieve a successful separation of enantiomers. The theoretical part of the thesis focuses on the analysis of the basic principles of high-performance liquid chromatography, the importance of optical isomerism, the basic principles of chiral separations and introduction of borane clusters together with the possibilities of their usege in modern pharmacotherapy. The practical part of the thesis focuses on experimental assessment of...
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Proposal to Change the Marketing Communication of a Real Estate Agency
Kolářová, Anna ; Kučera, Radim (referee) ; Kaňovská, Lucie (advisor)
This thesis deals with a proposal to improve the marketing communication of a selected real estate agency with a primary focus on the preferences of Generation Z. The thesis is divided into three parts, the theoretical part focuses on marketing communication of services, generation Z, X and Y and the main features characterizing the real estate market. The analytical part focuses on the current situation of the selected real estate agency in the field of marketing communication, the analysis of the external and internal environment and qualitative research focusing on the preferences of Generation Z in choosing their own housing. In the proposal part, optimal changes in the field of marketing communication for the real estate agency are recommended on the basis of the analytical part.
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Detached house with shop of cloths and haberdashery in Praha - Libuš
Dvořáková, Hana ; Kučera, Radim (referee) ; Štěpánek, Ladislav (advisor)
The bachelor thesis is a project of a multi-storey detached house with shop of cloth and haberdashery in Prague. The house is designed for two families. The shop is located in the 1st floor and is functionally completely independent of the operation of the residential part. The entrance of the shop is located on the main street. The entrance to the residential part is on side street. The rooms are oriented to the southwest. The building has walls made of ceramic blocks Porotherm, the ceiling and the stairs are monolithic reinforced concrete. The project was worked out in a training version of Autocad, the editions were processed in the Archicad program. During processing the emphasis was on architectural and layout solutions, static requirements and safety in use.
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Detached House
Slavotínková, Radka ; Kučera, Radim (referee) ; Smolka, Radim (advisor)
This bachelor’s thesis deals with the design documentation of a detached house for two families. The house is situated in the district Slavonín in Olomouc city, catastral district Slavonín. The supporting structures of building is designed in the integrated building system Porotherm. The main building and both garages are roofed by shed and double-shell roof. Construction of roof is made like purlin system from wood components. The buildings has two floors abobe ground.
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Detached house with a coffee bar in Kroměříž
Skopalová, Vendula ; Kučera, Radim (referee) ; Štěpánek, Ladislav (advisor)
The subject of this bachelor's thesis is to design and process a construction-technical part of construction realisation documents of a new family house with two flats and a café in Kroměříž. The building is located on a flat land and comprises of a partial basement and three above ground storeys. A garage for both flats is designed in the project. The building is covered by a saddleback roof with concrete roofing. Vertical load bearing structures are made of the Porotherm system. In addition to its own project, it also includes an architectural conception, fire safety report and thermal and technical assessment of the house.
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Yacht Club Hlucin
Kučera, Radim ; Šuhajdová, Eva (referee) ; Šuhajda, Karel (advisor)
The aim of this study is the design of Yacht club. The building is situated on a building estate No. 1303/3 of the Kozmice land registry in the recreational premises at the lakefront of „Hlučínské jezero“. It is placed next to the flooding line which is also considered in the project. The building is divided into three operational parts – the hotel, the catering establishments (restaurant) and the area primarily destined for holding conferences and workshops. The hotel is designed to accommodate thirty-two people, the capacity of restaurant is forty-two and conferential area is suitable for forty people at the most. Yacht club is designed as four-storey building with a flat grassed-covered roof. With regard to the foundation conditions, the building is found on piles. The structural part of walls is partly from CLT panels and partly from reinforced concrete which increase the stiffness of the building. The external cladding of the hotel consists of wooden blocks creating ventilated facade, while the rest of the building is rendered.
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Guesthouse
Vlčková, Bára ; Kučera, Radim (referee) ; Pěnčík, Jan (advisor)
This bachelor thesis is a project of new five-storey, semi basement guesthouse in Opava. This guesthouse will be used for accommodation, catering and recreation. Accommodation capacity is 21 people. In the basement is a technical background. The first floor is designed for the overall run of the guesthouse, staff, catering and sports. In the second and third floor are rooms for guests. Almost every room has a balcony. In the fourth floor is a common room with adjoining terrace. The building is brick. The vertical structures are made of ceramic blocks. Outer walls are insulated by outer contact system. The ceilings are mostly ceramic-concrete and a smaller part of the reinforced concrete. The guesthouse is roofed by single-flat roof.
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Detached house with a design office
Spáčilová, Kristýna ; Kučera, Radim (referee) ; Kolář, Radim (advisor)
This bachelor thesis deals with the design and processing of the design documentation for the construction of a new detached house with a design office, which is located in the cadastral unit of the village of Výkleky on plot no 79/1; 79/2. The house is divided into dwelling unit and establishment. The object is designed as a double floor and partly basement. The house is roofed with hipped roof. Construction systém wall, brick from brick´s blocks, basement is from permanent forwork. The bachelor thesis is elaborated in the form of project documentation for construction.
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