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Derivatives of pyrazinecarboxylic acid as potential antituberculotics (synthesis and biological evaluation)
Vaňásková, Barbora ; Doležal, Martin (advisor) ; Zimčík, Petr (referee) ; Malík, Ivan (referee)
Charles University in Prague, Faculty of Pharmacy v Hradci Králové Department: Department of Pharmaceutical Chemistry and Drug Control Candidate: Mgr. Barbora Vaňásková Supervisor: Prof. PharmDr. Martin Doležal, Ph.D. Title of Doctoral Thesis: Derivatives of pyrazinecarboxylic acid as potential antituberculotics (synthesis and biological evaluation) This doctoral thesis deals with searching for potential antituberculotic drugs derived from pyrazinecarboxylic acid. Thesis contains theoretical part, in which problematics of tuberculosis, factors hindering the effectiveness of treatment (development of resistance and HIV coinfection) and current therapeutic practice are outlined. An individual chapter is devoted to the composition of the mycobacterial cell wall. A brief overview of first-line and second-line antituberculars as well as drugs newly introduced into the clinical practice and promising derivatives in various phases of preclinical and clinical trials is further stated. Special attention is dedicated to pyrazinamide, current theories dealing with mechanism of action of this first-line antituberculotic drug and to ribosomal protein S1, a specific target of pyrazinecarboxylic acid. A summary of pyrazinamide derivatives with antimycobacterial activity published since 2011 is listed for...
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Spatial plastic creation in Changing concepts of art education : ceramic art as a phenomenon of visual arts and art education
Woolf, Karolina
Rozvíjení trojdimenzionálního - prostorového - myšlení, které je důležité pro poznávání světa a pochopení osobní identity v něm, je důvodem k častějšímu prosazování prostorové tvorby ve výuce na základních školách. Tato identifikace by měla probíhat na základě tvůrčích aktivit podmíněných poznávací hodnotou celistvosti lidského zážitku. Ohniskem pohledu by mělo být vzájemné doplňování prostorového a plošného vyjadřování, přičemž diferenciace tkví ve vymezení pólů trojdimenzionální a dvojdimenzionální formace. Stává se ale, že při rozlišování obou útvarů ve výuce dochází k omylům, které hovoří o nedostatečném pochopení či úplné desinterpretaci problému způsobu vyjadřování. Zároveň se ukazuje, že preference plošné tvorby a distance od prostorové tvorby ve výuce je velmi častá. Příčinou se zdá být technologická náročnost prostorové tvorby (v přímé úměrnosti s časovou), která souvisí s výtvarnou průpravou pedagogů. Hlavním zaměřením mého odborného zájmu i obsahu mé disertační práce je prostorová plastická tvorba, její kvalitativní a kvantitativní zastoupení ve výuce výtvarné výchovy na primárním stupni základní školy. Domnívám se, že souvztažnost kvality a kvantity prostorové tvorby souvisí s pregraduální přípravou studentů - učitelů a s jejich oborovým zaměřením. Powered by TCPDF (www.tcpdf.org)
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Use of bioproducts in public catering systems in Czech Republoc and Austria
KOSTKOVÁ, Miroslava
The paper studied the structure of meals in selected restaurants in the Czech Republic and compared with selected Austrian catering facilities. The analysis shows that Austria is against the Czech Republic ahead of not only the quantity used in organic food, but also in the knowledge that is related to organic food. And not just in public catering facilities, but also in households. In the questionnaire survey was to determine knowledge about organic foods, the principles under which they were prepared, where you can buy at what price range varies. About the quality of organic food, people's interest in organic food, organic food as often used in homes both Czech and Austrian. Were also detected in the possibilities of school catering facilities, the reasons why organic food is often used and more. All of this was examined children's nursery school, primary school pupils and college students and executives interviewed kitchen. The result is that in the Czech Republic are used almost exclusively organic foods at home and rarely. While in the kitchens of school facilities for them is great interest either from the kitchen diners and employees. By contrast, in Austria, organic food is commonly used both in households and in public catering facilities and thein use is considered an asset. SWOT analysis derived from several sources provided by the Ministry of Agriculture, shows the appropriateness of inclusion of organic food to offer menus. Understanding the concept of organic food is gradually increasing, from our survey suggests that this concept students know 72% and 75% of staff kitchen. In Austria, this question knew the answer 100% of the respondents. 13% of respondents would welcome the offer of meals of organic foods in their cafeterias, dining halls in the Austrian would appreciate higher proportion of organic food. 60% of students in the questionnaire said that they can byu organic food in supermarkets, while in Austria prevails buy organic food directly on the farm. Most in the Czech Republic to sign purchase organic fruits and vegetables, in second place as milk and dairy products. In contrast to Austria, where most purchases organic milk and dairy products, fruit in second place and third place is vegetables.
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Antituberculosis Agents and Their Antimicrobial Effects.
Novotná, Eva ; Waisser, Karel (advisor) ; Kvasničková, Eva (referee) ; Lešetický, Ladislav (referee)
Charles University in Prague, Faculty of Pharmacy in Hradec Králové Department of Organic and Inorganic Chemistry Candidate: Mgr. Eva Petrlíková Supervisor: Prof. RNDr. Karel Waisser, DrSc. Title of Doctoral Thesis: Antituberculosis Agents and Their Antimicrobial Effects. The dissertation focuses on the preparation of antimycobacterially active compounds. Some of the prepared compounds were also screened for the in vitro antibacterial and antifungal activity. The prepared compounds included sulfur derivatives of 3-benzyl-2H-1,3-benzoxazine- 2,4(3H)-diones, N-(pyridylmethyl)salicylamides, sulfur derivatives of 3-(4-alkylphenyl)- 2H-1,3-benzoxazine-2,4(3H)-diones, N-benzylthiosalicylamides, benzaldehyde- Sbenzylisothiosemicarbazones, salicylaldehyde-S-benzylisothiosemicarbazones, derivatives of 1,2-bis(9H-fluoren-9-ylidene)-N,N'-diarylethane-1,2-diamine, and hybrid molecules of cholesterol and terpenes. The highest antimycobacterial activity was exerted by 3-benzyl-2H-1,3-benzoxazine- 2,4(3H)-dithione and 3-(3,4-dichlorobenzyl)-2H-1,3-benzoxazine-2,4(3H)-dithione, 3-(4- secbutylphenyl)- 7-methyl-4-thioxo-2H-1,3-benzoxazine-2(3H)-one, N-(4-methylbenzyl) thiosalicylamide and 4-methyl-N-(4-methylbenzyl)thiosalicylamide. Salicylaldehyde- S-(4-chlorobenzyl)isothiosemicarbazone was the most active...
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Healthy Life Style Influence on Civilization Diseases Prevention
Svěráková, Dagmar ; Novotná, Viléma (advisor) ; Holá, Iveta (referee)
Název: Vliv zdravého životního stylu na prevenci civilizačních chorob. Healthy life style's influence on civilization diseases prevention. Cíl práce: Posouzení životního stylu cvičenců hromadné pohybové skladby Pohoda v průběhu přípravy na Světovou gymnaestrádu v r. 2007 a dále výběr a souhrn poznatků o případných zdravotních ohrožení vyplývajících ze zjištěných somatických údajů a dotazníkového šetření. Metoda: Výzkum byl prováděn formou dotazníkového šetření a antropometrickým měřením se 346 respondenty, kteří se zúčastnili nácviků hromadné pohybové skladby Pohoda (15.10 2005. - 18.6. 2006). Zastoupeny byly ženy i muži různých věkových kategorií. Výsledky: Budou sloužit jako východisko k dalšímu zkoumání v rámci výzkumných úkolů zaměřených zejména na program boje proti civilizačním nemocem, proti obezitě a na rozšíření nabídky vhodných pohybových aktivit pro dospělou populaci a seniory. Klíčová slova: Zdravý životní styl, wellness, srdečně - cévní onemocnění, obezita, hypertenze, diabetes mellitus, dyslipidémie, nekuřáctví, pohybová aktivita.
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Use of the extrusion process to produce biogas from wheat straw
VERNER, Dušan
Many agricultural biogas stations process predominantly phytomass specifically grown for power engineering purposes as a primary raw material. This results in gradual increase of maize proportion in sowing sequences at the exclusion of traditional area-specific crops, which presents various potential negative effects. The aim of study is to evaluate the substitution of maize with wheat straw in the anaerobic fermentation process from the biotechnological and economic viewpoint. For this purpose, wheat straw pellets were pretreated using the high-pressure extruder in compliance with UV CZ 21314 at different runtime parameters. Cumulative methane (CH4) production in quarter-mode operation simulation, based on the extrusion pressure, cycle duration and fermentation temperature, was the main evaluation criteria. Optimal run time parameters were derived from the approximation ? extrusion pressure 1,35 MPa, reaction time 210 s, in order to achieve maximal CH4 production at mesophilic fermentation temperature (38 °C). For fermentation temperature 48 °C, optimal pressure 1,25 MPa and cycle duration 180 s were approximated. The discount rate of Net Present Value (NPV) was established as a main comparative criterion considering overall executive, legislative and technological aspects of analyzed biological effects. Based on these findings suggest, wheat straw extrusion is interesting, unconventional and profitable technology in the field of biogas production.
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Activities For Listening to Music at Primary Schools
Roubíčková, Olga ; Váňová, Hana (referee) ; Hurníková, Kateřina (advisor)
The dissertation submits the theoretical elaboration about the problem o f listening activities in terms o f music education in primary school. Listening of music is an integral part o f music education in primary school. Its function is essential for this type o f education. Effectiveness o f listening activities in primary school depends on many factors which were examined from their functional point o f view. Requests o f an active form o f listening and related listening activities raise a question to what extend the music education text books deal with this problem. The text books were analysed in terms of listening activities problem and based on that the suggestion of listening repertory was created, supplemented with the methodical process of work. The individual examples were chosen, concerning music abilities and skills o f pupils attending the primary school. Creativity is the base for the music thinking development. Methods for cultivating the music creativity are the important part of education. Cooperative education, project method and use o f information technology in music education are the methods which help to develop pupil's music creativity. The other part of this dissertation is the suggestion for the way o f work with those methods developing the music creativity, related to listening...
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Study of cytotoxicity of potential antituberculotics using selected methods on liver and kidney cell line
Katrnošková, Simona ; Ramos Mandíková, Jana (advisor) ; Bárta, Pavel (referee)
Charles University Faculty of Pharmacy in Hradec Králové Department of Pharmacology and Toxicology Student: Mgr. Simona Katrnošková Supervisor: PharmDr. Jana Ramos Mandíková, Ph.D. Title of Thesis: Study of cytotoxicity of potential antituberculotics using selected methods on liver and kidney cell line During pharmacologic therapy, tissues of liver and kidney are frequently exposed to high doses of xenobiotics. Via in vitro assays during preclinical testing, we are able to predict potential toxicity which helps to prevent the possible serious adverse drug reactions in clinical practice. The aim of this rigorous thesis was to state the cytotoxic profile of 4 potential antituberculotic drug candidates using appropriate cell models and in vitro assays. Another aim was to compare the cytotoxic effect of the tested compounds among themselves and to 4-aminosalicylic acid (PAS) which antituberculotic activity is known for many years. The tested substances were 3 salicylanilide diethyl phosphate-based derivatives and 4-(trifluormethyl)benzoic acid. For the cytotoxic potential assessment, we used the parameter half maximal inhibitory concentration IC50. We have used methods determining the cell metabolic activity, aminopeptidase activity, lactate dehydrogenase leakage and activity of 3/7 caspases in this...
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The synthesis of substituted pyridines employing gold(I) catalyst
Janoušek, Martin ; Špulák, Marcel (advisor) ; Kuneš, Jiří (referee)
Charles University in Prague Faculty of Pharmacy in Hradec Králové Department of Inorganic and Organic Chemistry Candidate: Martin Janoušek Supervisor: PharmDr. Marcel Špulák, Ph.D. Title of thesis: The synthesis of substituted pyridines employing gold(I) catalyst This work is focused on the preparation of 3,4-disubstituted pyridine derivatives. MBS- protected propargylamine and MS-protected 1-ethynylcyklohexylamine provide with methyl propiolate to form appropriate 1,5-enyne, which undergoes Sonogashira coupling with various aryl iodides. Substituted enyne is subjected to cyclization yielding appropriate tetrahydropyridine in the presence of catalyst tris(2-furyl)phosphinegold(I) chloride. Derivate substituted by pentamethylen-1,5-diyl didn't cyclize. Deprotection leads to the preparation of substituted pyridines, which could serve as an intermediates in organic synthesis or potentially with biological activity. Keywords: gold catalysis, enyne cyclization, pyridine derivatives
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