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Pyrazine derivatives as potential drugs I
Sedlák, Petr ; Doležal, Martin (advisor) ; Miletín, Miroslav (referee)
Title of diploma thesis: Pyrazine derivates as potential drugs I. Review of tuberculosis therapy and modern research were presented in this diploma thesis. Novel pyrazine derivates connected via CO-NH-NH- bridge with substituted phenyl derivates were synthesized. Novel structures were characterized by melting points, TLC, IR, 1H and 13C NMR. This set was put through in vitro biological evaluation. Log P and Clog P were also calculated and were compared with novel synthesized structures.
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Derivates of Pyrazine as potentional drugs III.
Gryc, Michal ; Doležal, Martin (advisor) ; Zimčík, Petr (referee)
Title of the diploma thesis: Derivates of Pyrazine as potentional drugs III. Within this thesis the research focused on the current influence of tuberculosis in the world was carried out as well as its therapy. In the chemical literature, there were found some methods to prepare the substituted esters of pyrazincarboxylic acid. There was synthesized six substances of the character like esters pyrazincarboxylic acid, that had not been described so far. The compounds were synthesized in the CEM Discover microwave system with Explorer 24 autosampler and purified and separated using a CombiFlash ® Rf. Device. All the products were characterized by melting point, TLC, IR, 1 H, 13 C NMR spectra. Series of substances were subjected to in vitro biological evaluation. The work result brings some new information on the antimycobacterial activity. In addition, the calculated log P values of newly prepared compounds are also presented in this thesis.
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Pyrazine derivates as potential drugs IV.
Schürger, Oliver ; Doležal, Martin (advisor) ; Miletín, Miroslav (referee)
Oliver Schürger: Pyrazine derivates as potential drugs IV. Keywords : tuberculosis, Mycobacterium tuberculosis, Directly Observed Treatment Strategy, Multi drug Resistence, pyrazinamide Abstract of Diploma Thesis: This review is about worldwide problem of tuberculosis and about new trends in its treatment. Also chemical search about methods of preparing substituted amides of pyrazinecarboxylic acid and pyrazine-2,5-dinitril was done. All products were characterized by melting point, TLC, elemental analysis, IR analysis, log P and some of the final products have also 1 H, 13 C NMR spectra made. Products were not been tested in biological studies yet.
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Pyrazine derivates as potential drugs III.
Bielesz, Stanislav ; Doležal, Martin (advisor) ; Chlupáčová, Marta (referee)
Derivates of pyrazine as potential drugs III Degree paper Stanislav Bielesz Charles University in Prague, Faculty of Pharmacy in Hradec Králové, Department of Pharmaceutical Chemistry and Drug Control, Heyrovského 1203, Hradec Králové The aim of this degree paper was to synthetise a series of derivates of pyrazine-2-carboxylic acid. In the concrete it was the series of substituated 3-phenylaminopyrazine-2,5- dicarboxamides. The substances were synthetised by common synthesis, they were characterised by their physiochemical properties (melting point, lipophility), IR spectroscopy and 1 H and 13 C NMR spectroscopy. The synthetised substancies were tested in USA for anti-tubercular activity by TAACF. The results of in vitro testing were good, but not enough for the further testing in vivo. They were also tested on the Faculty of Pharmacy against fungi. No activity was found.
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Synthesis of zinc (II) aryloxy azaphthalocyanines
Vůjtěch, Petr ; Zimčík, Petr (advisor) ; Doležal, Martin (referee)
SYNTHESIS OF ZINC (II) ARYLOXY AZAPHTHALOCYANINES Petr Vujtech Department of Pharmaceutical Chemistry and Drug Control, Faculty of Pharmacy in Hradec Kralove, Charles University in Prague The aim of my diploma thesis was synthesis of azaphthalocyanine (AzaPc) derivate which should be free of aggregation. The aggregation is unfavorable property of AzaPc that reduces the singlet oxygen quantum yield. There are several methods to increase the ratio monomer/aggregates. The most effective strategy involves the use of bulky substituents attached to the AzaPc`s periphery. That is why, 2,3,9,10,16,17,23,24-octa(2,6-di-iso-propyphenoxy)- 1,4,8,11,15,18,22,25-octaazaphthalocyaninato zinc(II) was prepared. Alkoxides cannot be used for cycloteramerization of aryloxy derivatives due to the well-described transetherification problems. Cyclizations in dichlorobenzene and quinoline with zinc(II) acetate were unsuccessful. Some AzaPc products appeared in reactions performed with zinc(II)acetate in pyridine or dimethylformamide, but the yields were small and the products were not perfectly pure. The best way to synthesis of aryloxy derivatives of AzaPc is reaction with Zn(quinoline)2Cl2 in a melt. Temperature of the mixture should be around 260 řC. Lower temperature causes the mixture does not react totally while the product...
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Conjugates of oligonucleotides with photodynamic or fluorescence quenching azaphthalocyanine molecules.
Göringerová, Hana ; Miletín, Miroslav (advisor) ; Doležal, Martin (referee)
Charles University in Prague Faculty of Pharmacy in Hradec Králové Department of Pharmaceutical Chemistry and Drug Control Diploma thesis Conjugates of oligonucleotides with photodynamic or fluorescence quenching azaphthalocyanine molecules Author: Hana Göringerová Supervisor: PharmDr. Miroslav Miletín PhD. This thesis deals with possibilities of creating conjugates of oligonucleotides with photodynamic or fluorescence quenching azaphthalocyanine molecules. We created this conjugates by using Copper (I)-catalyzed Huisgen 1,3-dipolar cycloadditions of terminal alkynes and azides which is the most often used method of click chemistry. Oligonucleotides on solid phase with sequence of 25T modified by hexynyl were utilized during this reaction. These oligonucleotides on solid phase reacted with P14-1Zn dye with CuI as catalyst and THF (DMSO) as a solvent. Products of this reaction were characterized by UV-VIS spectrophotometer and MALDI-TOF analysis. Others procedures which were made within our thesis, turn out to be unsuccessful. The problem was that the dye did not conjugate to oligonucleotides on solid phase.
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Principles and Methods of social work with Social Groups in training housing regarding to Method of Sanation of Family in social Exclusion.
Doležal, Martin ; Vorlová, Marie (advisor) ; Poláčková, Iva (referee)
This Bachelor work is focused on principals and methods of social work in the higher type of asylum accommodation, which is called House of Training Accommodation. I want to introduce new model of social accommodation and social work for 21. century, with all social classes and groups. This new type of asylum accommodation is serving like an instrument of sanation of family and other pathological appearances in the society, for example unemployment, drug addiction and prevention of heavy crime, homeless and insufficient finantial situation for living, insolvency, rasial discrimination and defense of those clients who are in senior old age with pension income. This work will be focused on concrete objects of social work in the training house: with leaver of creches, applicants to senior homes, 5 clients coming from regime of serving a sentence (VTOS), single mothers with their children or women under domestic and elderly abuse and violence, ethnical minorities and famillies. At the end of this written bachelor work I wish to show compatibility of this type of social work with standards of quality of social work, especially with standards no. 3. and 5., which are the main pillars for the success of social work in the higher asylum accommodation. One chapter also shows problematic point of issue of social work...
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Structure-Antifungal Activity Relationships in Substituted Butenolides
Šenel, Petr ; Pour, Milan (advisor) ; Hampl, František (referee) ; Doležal, Martin (referee)
Within the framework of this Thesis, several series of 3-(4-bromophenyl)-2,5- -dihydrofuran-2-ones with various substituents at C(5) derived from in vitro antifungally active 3-(4-bromophenyl)-5-acetyloxymethyl-2,5-dihydrofuran-2-one were prepared with the aim of further development of potential antifungals based on this lead. Primarily, we focused on the synthesis of furanones bearing alkylidene or alkoxymethyl/aryloxymethyl moiety in position 5. We found that 5-acyloxymethyl and 5-aryloxymethyl furanone derivatives undergo elimination leading to 3-(4-bromophenyl)-5-methylene-2,5-dihydrofuran-2-one under the antifungal screening conditions. This compound initiates fungal cell membrane disruption and is responsible for the antifungal activity of the former. The 5-alkoxymethyl analogues are unable to undergo the elimination process and are therefore inactive. The antifungal activity of 5- alkylidene furanones depends on the substitution of alkylidene side chain. Some of the target compounds displayed interesting cytostatic activities against HeLa S3 and CCRF-CEM cells (IC50 < 5 µmol.L-1 ). Furthermore, syntheses of 4-substituted or 4,5-disubstituted-3-(4-bromophenyl)-2,5- -dihydrofuran-2-ones were carried out. Some of the prepared derivatives possessed notable antifungal or antimicrobial activity.
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