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Design of the Tractor's front axle drive
Podhora, David ; Krátký, Martin (referee) ; Prokop, Aleš (advisor)
This master’s thesis is deal with the design of the tractor’s front axle drive to enlarge its braking efficiency of the standing tractor fixed by the parking brake. In the first two chapters, the basic information related to the above stated issue is being summarized. Next, procedure of creating the design including the fundamental calculation proposal is being described. In the last chapter, the strain-stress analysis of the selected partial sections of the design is being presented. The final design is supported with the drawing documentation that is being part of this master’s thesis, too.
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Calculations of parameters of biologically active compounds by the quantum mechanical methods.
Horáček, Ondřej ; Palát, Karel (advisor) ; Krátký, Martin (referee)
8 ABSTRACT The aim of this work is to calculate the parameters of substituted bases and chosen phenylguanidinium cations, earlier synthesized at the Department of inorganic and organic chemistry on the Faculty of Pharmacy CU in Hradec Králové, using quantum chemical methods. I solved chosen problem by using computer programs Gaussian 03W and Hyperchem 8.0.10. I used program Gaussian to optimize the molecules and calculate the energy of the HOMO and LUMO, total energy and the atomic partial charge using the Mulliken population analysis. I used programe HyperChem to calculate the Van der Waals molecular volume; Van der Waals molecular surface; logP; the molar refraction; solvent-accessible surface of the probe size 1.0 Å; 1.2 Å; 1.4 Å; 1.6 Å and the atomic partial charge using methods PEOE. All parameters of selected substituted phenylguanidines above have been successfully calculated, and listed in the tables in the chapter called results. The calculated results were discussed in chapter called discussion. The calculated parameters will be used for further correlations and QSAR studies that will help to understand the biological activity of substituted phenylguanidines and hence their effect on the human organism.
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Synthesis of antimicrobial compounds based on derivatives of salicylic acid
Tvrdý, Václav ; Krátký, Martin (advisor) ; Vinšová, Jarmila (referee)
Schiff bases are widely used both in technical practice and in the field of medicine. For their antimicrobial activities are studied as potential antimacterial and abtifungal drugs. With increasing level of resistence to currently drugs is the development of new substances very intense. Salicylanilides are a group of substances with antimicrobial activity and are also intensively studied. Based on that we were synthesized novel Schiff bases resulting from salicylic acid, respectively salicylanilides. It was concretely prepared five compounds: 5- chloro-N-{4-[phenyl(phenylimino)methyl]phenyl}-2-hydroxybenzamide, 5-bromo-N-{4-[ phenyl(phenylimino)methyl]phenyl}-2-hydroxybenzamide, 5-chloro-N-{4-[phenyl(3- chlorfenylimino)methyl]phenyl}-2-hydroxybenzamide, 5-chloro-N-{4-[phenyl(4- chlorfenylimino)methyl]phenyl}-2-hydroxybenzamide, 5-bromo-N-{4-[phenyl(4- chlorfenylimino)methyl]phenyl}-2-hydroxybenzamide. The reaction proceeded at the boiling point of the solvent, with catalytic amount of p-toluensulfonic acid. Most of the compounds were characterized by IR, H1 NMR, C13 NMR and melting point. The prepared compounds showed E/Z isomers on double bond, it is demonstrated on NMR specters.
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Modification of antimycobacterial active sulphonamides
Kufa, Martin ; Krátký, Martin (advisor) ; Vinšová, Jarmila (referee)
The importance of the searching for novel antimycobacterial active agents is continually increasing with growing mycobacterial resistance to currently used drugs. However, the resistance-related problems are also associated with other bacteria and fungi. The systematic modification of compounds with a known antimicrobial activity represents one of the possible approaches to overcome this problem. Sulphonamide derivatives may be considered to be such a kind of compounds. That is why we synthesized various sulphathiazole derivatives. Amides were obtained by the reaction of sulphathiazole with appropriate acyl chlorides, substituted ureas from corresponding isocyanates. These ureas were cyclized via oxalyl chloride to form substituted 2,4,5-trioxoimidazolidines. Among derivatives evaluated for their antimycobacterial action, 4-(3- phenethylureido)-N-(thiazol-2-yl)benzenesulphonamide showed the highest activity. Its minimum inhibitory concentrations (MIC) against Mycobacterium tuberculosis My 331/88 (4 µmol/l) were superior to those obtained for sulphathiazole. In the case of nontuberculous mycobacteria (M. avium My 330/88, M. kansasii My 235/88 and M. kansasii My 6509/96), their activities were comparable (≥ 2 µmol/l). Amides showed also a significant antimycobacterial activity, especially against M....
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Synthesis of salicylanilide esters active against MDR-TB
Vosátka, Rudolf ; Vinšová, Jarmila (advisor) ; Krátký, Martin (referee)
VOSÁTKA, Rudolf., Synthesis of salicylanilide esters active against MDR-TB, Hradec Králové: Faculty of Pharmacy of Charles University, 2013, 54 s, Diploma thesis. This diploma thesis deals with the synthesis and activity of salicylanilides and their esters against MDR-TB. Specifically, 4-bromo-3-(trifluoromethyl) aniline, 3,5-bis (trifluoromethyl) aniline and their esters as isonicotinates, pyrazincarboxylates and 1H- imidazole-4-carboxylates. Moreover, there is also 5-chloro-N-(3,4-dichlorophenyl)-2- hydroxybenzamide, which inter alia demonstrates the best MIC compared to other synthesized substances. Thesis summarizes problems of tuberculosis, its current treatment and supplementing to the current trend in the development and research on specific examples of potential drugs. Much of this thesis deals with salicylanilides.
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Synthesis of novel isoniazid derivatives
Rychtarčíková, Zuzana ; Vinšová, Jarmila (advisor) ; Krátký, Martin (referee)
TB remains a major cause of population mortality in the world. Research of new substances with antimycobacterial activity is emphasized also because of increasing occurrence of resistance in case of monotherapy as well as combination therapy with AT of first and second line. Current trends in the development rest in the connection of two molecules into one - the so-called double active compound - by means of various linkers. In the process of synthesis of 2-isonicotinoyl-N-substituted phenylhydra- zinecarboxamides, a carbonyl bridge was used. The synthesis of these substances was realized by two methods. In the first one, the reaction was based on substituted isocyanate; in the second one, preparation of isocyanate in situ from a substituted aniline using triphosgene was applied. All substances were tested for in vitro antimycobacterial activity. The substance 2-isonicotinoyl-N-(2,4,6-trichlorophenyl)hy- drazinecarboxamide exhibited the highest activity against Mycobacterium tuberculosis 331/88 with MIC value (4 μmol/L). The compounds were also tested for other strains of mycobacteria - Mycobacterium avium 330/88, Mycobacterium kansasii 235/80 and Mycobacterium kansasii 6509/96. Synthesis of N-substituted phenyl-5-(pyridine-4-yl)- 1,3,4-oxa-diazol-2-amines was based on the selected and prepared...
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The use of laser microdissection for the genotyping of biological material isolated during an abortion.
Beranová, Karina ; Krátký, Martin (advisor) ; Kopečný, Michal (referee)
The use of laser microdissection for the genotyping of biological material isolated during an abortion Abstract In forensic genetics laser microdissection is used mainly as a method of cell separation from samples of mixed biological traits of sexually motivated crimes. It can also be used in paternity testing via genotyping of biological material isolated during an abortion. The foetal part of placenta is separated from the acquired samples and a pure DNA profile of the foetus is determited. This DNA can be compared to the suspect's DNA. The goal of this project is the application of laser microdissection to separate chorionic villi from a placenta and the subsequent genetic analysis leading to the determination of a pure foetal DNA profile. A secondary goal was the preparation and optimization of the method necessary for its introduction to forensic practice. In the first phase the optimization of the sample preparation was conducted on test sections of muscular tissue and epithelial cells from a buccal swap. Experimental material acquired during abortions of voluntary donors was used in the second phase. This technique was simultaneously tested on material directly linked to criminal acts. The separation of 10 chorionic villi cells with the method of laser microdissection eventually resulted in the...
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