National Repository of Grey Literature 74 records found  beginprevious20 - 29nextend  jump to record: Search took 0.00 seconds. 
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....
Influence of benzoxazinedione derivatives on selected mycobacterial enzymes
Švidrnochová, Michaela ; Novotná, Eva (advisor) ; Krátký, Martin (referee)
Charles University in Prague Faculty of Pharmacy in Hradec Králové Department of Biochemical Sciences Candidate: Mgr. Michaela Švidrnochová Supervisor: RNDr. Eva Novotná, Ph.D. Title of Thesis: Influence of benzoxazinedione derivatives on selected mycobacterial enzymes Tuberculosis is an insidious infectious disease with more and more increasing incidence in certain regions. It is difficult to treat by the available means because of increasing cases of multidrug resistance, which is defined as a resistance of M. tuberculosis at least to two primary antituberculotic drugs - rifampicin and isoniazid. That's why is necessary to search for new substances which interfere with the metabolic pathways of Mycobakterium tuberculosis. Enzyme inhibitions in different levels of these pathways are considered to be a target of the new potencial antituberculotic drugs. In this work, influence of monosulphur and disulphur derivatives of 3-(4-alkylphenyl)-2H- 1,3-benzoxazine-2,4(3H)-dione on enoyl-ACP-reductase, dihydrofolate reductase, isocitrate lyase and FtsZ was tested by thermal shift assay, spectrofotometric method and light scattering. The results showed that the dihydrofolate reductase is not a drug target of selected inhibitors. Isocitrate lyase was the most inhibited by sulphur derivative 3-(4-terc-...
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...
Derivative of Aminobenzoic Acids as Potential Antimicrobial Agents
Brokešová, Kateřina ; Krátký, Martin (advisor) ; Janďourek, Ondřej (referee)
Charles University, Faculty of Pharmacy in Hradec Králové Department of Organic and Bioorganic Chemistry Candidate: Mgr. Kateřina Brokešová Consultant: PharmDr. Mgr. Martin Krátký, Ph.D. Title of Thesis: Derivatives of Aminobenzoic Acids as Potential Antimicrobial Agents The increasing resistance to previously unnecessarily used antimicrobial drugs has led to the need for search and synthesis of new drugs including Schiff bases. The rigorous thesis deals with the synthesis and subsequent characterization and evaluation of biological properties of new Schiff bases synthesized from substituted salicylaldehydes and aromatic amino acids and their derivatives (3-aminobenzoic, 3,5-diaminobenzoic acids and esters of 4-aminobenzoic acid). The prepared derivatives were evaluated for their antibacterial, antifungal and antimycobacterial activities; cytotoxicity was also investigated for the most active ones. Most of the Schiff bases exhibit antibacterial activity with minimum inhibitory concentration (MIC) from 7.81 µM, which is comparable with a standard drug bacitracin for some strains. Schiff bases appear to be more effective against Gram-positive bacteria including methicillin- resistant Staphylococcus aureus. The newly synthesized compounds are also effective against yeasts and filamentous fungi. The...
Synthesis of salicylanilide prodrugs
Krátký, Martin ; Vinšová, Jarmila (advisor) ; Imramovský, Aleš (referee)
KRÁTKÝ, Martin. Synthesis of Salicylanilide Prodrugs. Hradec Králové: Faculty of Pharmacy of Charles University, 2008. 75 pp. Diploma Thesis. This diploma thesis is concerned with synthesis of antibacterial prodrugs based on esters of salicylanilides with amino acids. First there are characterized prodrugs and their importance and then biological activities and application of salicylanilides. The main goal of this work was the synthesis of prodrugs of salicylanilides amino acids esters. Some synthesized compounds were evaluated especially for their activity against atypical Mycobacteria strains. These compounds possess antimycobacterial activity, but it is lower than initial salicylanilide 5-chloro- N-(3-chlorophenyl)-2-hydroxybenzamide. This diploma thesis acknowledges rearrangement after N-deprotection and α-amino group liberation of N-protected amino acids esters with salicylanilides to furnish diamides. The diamide was esterified by Z-amino acids (L-phenylalanine and glycine). These obtained esters were N- deprotected and the amino group was liberated. After this liberation there was described rearrangement to furnish probably triamides, analogously to furnishing of diamides. There are discussed two possible mechanisms of rearrangement - with forming of seven-membered benzoxazepinedione rings...
Laser microdissection in forensic genetics: genetic analysis of sexual abuse evidence
Faltýsková, Zuzana ; Krátký, Martin (advisor) ; Kopečný, Michal (referee)
Laser microdissection is a novel technique of cell separation under microscopic view utilizing a laser beam. It has been used for cell separation from mixed samples in forensic genetics, such as vaginal smear in cases of sexual assault. In a rape investigation, few cells are usually recovered as the only evidence available for the assailant identification. When analysing a resistant cell type such as sperms, an effective and reliable method is required. This study aims to optimise the genetic analysis of laser microdissected sperms and to take the optimal protocol into practice. The goal is to develop a technique capable of recovery of reliable genotyping results from just a few cells. Genetic analysis was optimised for sperms separated from pure semen samples by laser microdissection. After optimisation, it was validated for sperms recovered from a vaginal smear. In the resulting genetic profiles some artifacts occured, that have been reported in samples with low DNA content. Possible solutions of these artifacts occurrence and elimination are discussed. In conclusion, the developement of an efficient and reliable genetic analysis method was successful: 10 sperms were recovered from vaginal smear and the genotyping result was capable of individual identification of the sperm donor. Powered by TCPDF...
Synthesis and evaluation of human 6-hydroxyceramides
Majcher, Adam ; Opálka, Lukáš (advisor) ; Krátký, Martin (referee)
Title of the Master thesis: Synthesis and evaluation of human 6-hydroxyceramides Candidate: Adam Majcher Supervisor: PharmDr. Lukáš Opálka, Ph.D. Consultant: PharmDr. Andrej Kováčik, Ph.D. Charles University, Faculty of Pharmacy in Hradec Králové Skin Barrier Research Group, Department of Organic and Bioorganic Chemistry Ceramides (Cer), the members of sphingolipid family, occur in all human cells and play an important role in cell signaling. In high concentrations, Cer can also be found in the uppermost layer of epidermis called stratum corneum, along with free fatty acids and cholesterol (in equimolar ratio), where they form the intercellular multi-lamellar lipid matrix. The key function of stratum corneum is to ensure a permeability barrier, thus, to provide water and electrolyte homeostasis, and to prevent entry of harmful substances into the organism. Cer are composed of a sphingoid base and an acyl part derived from a long-chain fatty acid. Cer based on 6-hydroxysphingosine (H) are amongst the most unusual sphingolipids. In contrast to sphingosine-based Cer, 6-hydroxysphingosine-based Cer (H-Cer) are unique for the epidermis and, in addition, H-Cer are not typical for all mammals. Moreover, the function and biosynthesis of H-Cer in the skin is still not completely understood. Several...
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.

National Repository of Grey Literature : 74 records found   beginprevious20 - 29nextend  jump to record:
See also: similar author names
10 Kratký, Michal
1 Krátký, Marek
2 Krátký, Matouš
10 Krátký, Michal
1 Krátký, Milan
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