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Synthesis of acetylcholinesterase reactivators and their evaluation against the intoxications caused by the organophosphorus inhibitors in vitro.
Musílek, Kamil ; Doležal, Martin (advisor) ; Beneš, Luděk (referee) ; Bajgar, Jiří (referee)
6. Summary The Ph.D. thesis is focused on a development of the novel acetylcholinesterase reactivators - the causal treatment for the intoxications caused by the organophosphorus inhibitors of cholinesterases. The background for an experimental work was a review article based on the published papers in the period 1990-2004. The experimental work was focused on a synthesis, a structural analysis and an in vitro evaluation of the novel acetylcholinesterase reactivators, which were compared to the commercial available compounds. The structure activity relationship (SAR) studies of the novel acetylcholinesterase reactivators were prepared according to the in vitro results. Moreover, other novel acetylcholinesterase reactivators were synthesised based on the previous SAR data. Recently, some of the novel compounds are tested in vivo. In conclusion, it was prepared, determined and evaluated over than 70 novel acetylcholinesterase reactivators. The review and experimental papers (25 papers) were published in the scientific journals and presented as the short communications or posters at the scientific meetings in the Czech Republic or abroad.
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The influence of projects from Operational program "Podnikání a inovace" on the development of Tachov district
Žežulka, Martin ; Beneš, Luděk (advisor) ; Perlín, Radim (referee)
The influence of projects from Operational program "Podnikání a inovace" on the regional development of Tachov district The main goal of bachelor thesis is the research of influence of subsidies from operational program "Podnikání a inovace" on the regional development of Tachov district. The attention is engaged on description of peripheral Then there are promoted outlets of European regional policy including "operational programs" and their connection with czech developmental documents. Through impact of developmental projects on companies there is described influence of subsidies on local economy, particularly from standpoint of additional value. According to research there is described position of companies wthin value chains including influence of subsidies in upgrading of these positions. The main benefit of thesis is revelation of influence of research and development infrastructure on local economy and then, identification resources of another competitiveness. In additional there is designed recommendation for future local development. Key words: EU regional policy, regional development, Operational program "Podnikání a inovace", local economy
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Boundary conditions for stratified flows
Řezníček, Hynek ; Beneš, Luděk (advisor) ; Brechler, Josef (referee)
In this thesis is presented mathematical model of stratified 2D flow of viscous incopressible fluid and its program realization. Basic equations of fluid flow in Boussinesq approximation were solved by finite volume method on structured nonortogonal grid. Discretization was done by the principle of semi-discretisation. The space derivative was solved by AUSM me- thod with MUSCL velocity reconstruction. The viscid terms were solved through auxiliary grids. During time discretization artificial compressibility method was used in dual time. The resulting system of ODEs is integrated in time by a suitable Runge-Kutta multistage scheme. Numerical experiments were calculated for flow with Reynolds number equals 1000. Further 3 numerical experiments are presented with different boundary conditions. 1
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Synthesis of acetylcholinesterase reactivators and their evaluation against the intoxications caused by the organophosphorus inhibitors in vitro.
Musílek, Kamil ; Doležal, Martin (advisor) ; Beneš, Luděk (referee) ; Bajgar, Jiří (referee)
6. Summary The Ph.D. thesis is focused on a development of the novel acetylcholinesterase reactivators - the causal treatment for the intoxications caused by the organophosphorus inhibitors of cholinesterases. The background for an experimental work was a review article based on the published papers in the period 1990-2004. The experimental work was focused on a synthesis, a structural analysis and an in vitro evaluation of the novel acetylcholinesterase reactivators, which were compared to the commercial available compounds. The structure activity relationship (SAR) studies of the novel acetylcholinesterase reactivators were prepared according to the in vitro results. Moreover, other novel acetylcholinesterase reactivators were synthesised based on the previous SAR data. Recently, some of the novel compounds are tested in vivo. In conclusion, it was prepared, determined and evaluated over than 70 novel acetylcholinesterase reactivators. The review and experimental papers (25 papers) were published in the scientific journals and presented as the short communications or posters at the scientific meetings in the Czech Republic or abroad.
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Synthesis, study and structure activity relationships of antiinflammatory drugs derived from leukotriens
Junek, Richard ; Hartl, Jiří (advisor) ; Beneš, Luděk (referee) ; Kuchař, Miroslav (referee) ; Kuneš, Jiří (referee)
7 Summary A series of arylalkanoic acids derivatives bearing methyl(phenethyl)amino groups were prepared and their antileukotrienic activities involving LTB4 were evaluated. Regression analysis of the first group of derivatives of arylacetic acid has shown a strong dependence of these activities on lipophilicity for both LTB4 receptor binding and inhibition of LTB4 biosynthesis, parabolic relationships were derived. The values of slopes of the ascending linear parts of these dependences indicate various types of hydrophobic binding at the site of ligand interaction with relevant biomacromolecules. Regression analysis showed the slightly different parabolic dependences of this activity on lipophilicity of -methyl and -unsubstituted alkanoic acids derivatives. The relationship derived for -unsubstituted alkanoic acids extended by group of similar derivatives of arylacetic acids was without any change of regression coefficients and statistical criteria. It was concluded, that the most active compounds belong to 2-arylpropanoic acids derivatives with lipophilicity close to log Popt (= 6.98). The antiinflammatory effect of the compounds under study was evaluated in three animal models of inflammation and their possible utilization in the treatment of ulcerative colitis was followed. It can be stated that the...
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Isosters of transkarbams, synthesis, properties and biological activity
Holas, Tomáš ; Hrabálek, Alexandr (advisor) ; Sedlák, Miloš (referee) ; Beneš, Luděk (referee)
1. SUMMARY The major aim of this dissertation was to synthesize and test isosteric analogs of T12. On the whole, 76 new compounds were prepared which have not previously been published. 28 compounds were tested as the transdermal permeation enhancers. Structure of these synthesized compounds was confirmed by FTIR, 1 H NMR and 13 C NMR analysis. Purity of the carbamate salts was verified by CHN analysis. With respect to the results, financial and time demandingness, permeation-enhancing activity was measured only on selected compounds. More than 400 permeation experiments were performed, more than 3000 HPLC chromatograms were analysed. To sum up, the permeation studies have shown that there is the relationship between structure and action of the studied compounds in the middle-lipophilic donor medium. Permeation-enhancing activity from the 60% propyleneglycol donor medium is in the following order: ester carbonate ketone ≥ amide = carbamate = alkane. Furthermore, there have been found another arguments confirming proposed mechanism of action of T12 - CO2 release in stratum corneum.
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Adolescent needs of low-theshold club Oráč
BENEŠ, Luděk
The thesis deals with low-threshold youth work in the context of salesian pedagogy. Using secondary analysis examines the needs of adolescents recorded in official documents of low-threshold club Oráč. Needs are classified into the system of needs and research results are used to a comprehensive view of the declared needs of adolescents visiting low-threshold club of Salesian center in České Budějovice in 2012.
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Reality and Virtuality of Game in Postmodernism
BENEŠ, Luděk
The thesis focuses on virtuality and reality of game in history of human culture and on its recent pozition.The first chapter adresses reality and virtuality of game in traditional view definitions. The second chapter describes the evolution of culture in game since human origin to postmodernism and the evolution of game in art. The third chapter takes on the evolution and conditions of postmodern culture, and also game in postmodern art. Further it describes virtuality and reality of game and society nowadays. The fourth chapter again compares recent author's definitions of game and closes the thesis with resulting definition of virtuality and reality of postmodern game.
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