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Pyrazine derivatives as potential drugs I.
Plasová, Petra ; Doležal, Martin (advisor) ; Miletín, Miroslav (referee)
Title of diploma thesis: Pyrazine dervatives as potential drugs I. Presented by: Petra Plasová Tuberculosis belongs between wide-world spreaded infections diseases, by which is infected about one third of human population. Due to attempts with potencial pyrazine antituberculotics at our department of Pharmaceutical Chemistry were developed series of substituted arylaminopyrazines. The first one, 3-chloropyrazine derivate, provided via coupling (aminodehalogenation) with aromatic amine acquired compounds.Structure modifications was achived by changing of carboxylic functions groups, e.g. dehydrogenation of carboxamide (origin of carbonitrile) or by adition of monosulphane (originates carbothioamide). We gained 8 absolutely new substances, which have not been described before, so they were characterized by TLC, melting point, elementary analysis, IR, 1H,13C NMR spectrum and log P values. These new substances are under the testing in vitro of their activity, against Mycobacterium tuberculosis H37Rv under international research program for new antituberculotics testing (TAACF, USA), resultes are not known yet. Mentioned compounds were in vitro tested for antifungal activity against determine fungal pathogens on Departement of biological and medicinal sciencis and against four tribes of mycobacteria in...
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Decontamination of the large-scale facility
BURDA, Radek
The theoretical part of the thesis is divided in the five main chapters. First chapter generally defines the term ?contamination?, which is closely related to the decontamination. Second chapter is focused on the microbial contamination, defines infectious agents, the mechanisms of its spread and points out microbes most likely to be misused as a biological weapon. Third chapter of the theoretical part addresses the decontamination itself. It defines the decontamination in general aiming for microbial decontamination, i.e. the biological agent surface and environment removal. Two basic groups of decontamination e.g. physical and chemical procedures are mentioned in this chapter. Fourth chapter presents valid standards describing various types of examinations for the desinfecting preparations efficacy evaluation. The last chapter of the theoretical part covers large-scale facilities, defines them and describes experimental facilities at the Department of large-scale testing in the National institute for nuclear, chemical and biological protection in Kamenna. The aim of the thesis is to create own methodology of the disinfactant efficiency testing with emphasis on the real condition simulation. The decontamination was carried out by means of following methods: aerosol generator method, decontamination by evaporation, manual sprayer and engine sprayer respectively. For the analysis we chose these disinfactants: Chirosan? Plus, Incidin OxyDes, Kohrsolin? FF, Korsolex? basic, Persteril? 36 and Sanosil? Super 25 Ag. The disinfectant efficiency was tested in 30, 60 and 120 m3 facilities. The tested B-agents were: Bacillus anthracis, Bacillus atrophaeus, Escherichia coli, Staphylococcus aureus and Streptococcus pneumoniae. For the decontamination efficiency verification we used a modified surface assay, a modified suspension assay and an agarose assay. The following issues were of concern: We found out that, based on the analysis of different techniques of decontamination, the large-scale facility decontamination is feasible. The most effective method of decontamination appears the manual and engine spraying with the latter more convenient for spaces over the 30 m3 in the matter of time. The decontamination by evaporation was inefficient for the large-scale facility decontamination. Experiments revealed that method based on aerosol distribution is convenient for large-scale facility decontamination. However, the nature of decontaminating preparation has to be considered. All disinfactants tested have shown good bactericidal activity. Nevertheless, only Korsolex? basic a Persteril? 36 have shown sufficient sporicidal activity with equal effect. The disadvantage of the preparation Persteril? 36 is its significant corrosive activity, on the other hand is inexpensive. The preparation Korsolex? basic contains anticorrosive compounds, but is more expensive than Persteril? 36. Our results demonstrated that the most convenient method for the decomtamination of facilities up to the 30 m3 is the manual aerosol sprayer. For facilities of larger volume the engine sprayer decontamination is more convenient. From the preparations tested, only Korsolex? basic a Persteril? 36 are, with respect to advantages and disadvantages, usable in the Department of large-scale testing in the National institute for nuclear, chemical and biological protection in Kamenna.
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Synthesis and Biological Evaluation of Selected Polysubstituted Furanones
Kratochvíl, Jiří ; Opletalová, Veronika (referee) ; Pour, Milan (advisor)
The aim of this thesis was to prepare 5-(benzyloxymethyl)-3-(4-bromophenyl)-2,5- dihydrofuran-2-one derived from cytostatically active 5-alkoxymethyl-3-(4-bromophenyl)- 2,5-dihydrofuran-2-ones. However, none of the three proposed synthetic procedures led to the target molecule. Next we focused on the preparation of a series of 5-bis(acetyloxymethyl)-3- aryl-4-phenyl-2,5-dihydrofuran-2-ones with different aryl substitution derived from the antibacterially, antifungally and cytostatically active 5-bis(acetyloxymethyl)-3- (4-bromophenyl)-4-phenyl-2,5-dihydrofuran-2-one. The aim was to explore a relationship between aryl substitution in position 3 and biological activity of the compounds. The spectrum of products was also enriched by 5-acetyloxymethyl-3-aryl-4-phenyl-2,5-dihydrofuran-2-ones. In conclusion aryl substitution leads to a significant decrease or vanishing of the antibacterial, antifungal and cytostatic effects with the exception of 5-acetyloxymethyl-3-aryl-4-phenyl-2,5- dihydrofuran-2-ones, in which marginal antifungal (Absidia corymbifera), antibacterial (Staphycoccus aureus a Staphylococcus epidermidis) and significant cytostatic (L1210, HeLa S3, CCRF-CEM, IC50 < 5 µmol.l-1 ) activities were found.
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Quality of life of patients with stenosis of aortic valve
ŠVECOVÁ, Valentyna
This bachelor thesis is focused on the quality of life of patients operated for aortic valve stenosis. The aim of the thesis was to describe and compare the quality of the patients´ lives before the replacement of the native aortic valve with a mechanical or a biological valve to the state three months after the surgery. The research was done in the Cardio-Centre of the Hospital České Budějovice, a. s. The patients of the Cardio-Centre represented the studied group and were selected using the simple deliberate selection method. The research itself was done using the ?postal survey? method, i.e. without the assistance of the professional staff. Two hypotheses were established: Hypothesis 1 (H1): The quality of life of the patients suffering from aortic valve stenosis is negatively affected in the evaluated domains of HRQoL; Hypothesis 2 (H2): The quality of life of the patients with aortic valve stenosis is better three months after the surgery than before the surgery. Health related quality of life was studied using the quantitative research method based on the Short-Form SF-36 questionnaire, Generic type, in the HRQoL methodology in eight domains: physical functions, physical limitations in role activities, emotional limitations in role activities, physical and emotional limitations in social activities, pain, mental health, vitality, general perception of health status. The received data were converted into the electronic form using the related software that assessed the average score of the quality of life correlative of the state of health. The results before and after the replacement of the aortic valve were compared mutually and also to the international standard of HRQoL. The results have helped to prove that surgical replacement of the native aortic valve results in an improvement of the quality of the patients lives. It has been proved through the research that the quality of life had been improved in all domains, what confirmed the H2 hypothesis ? i.e. the quality of life of the patients with aortic valve stenosis is better three months after the surgery than before the surgery. It has been also discovered that the quality of life of the patients with aortal valve stenosis is significantly lower than the quality of life in health population represented by the results of the Oxford research. This confirmed the H1 hypothesis ? i.e. the quality of life of the patients suffering from aortic valve stenosis is negatively affected in the evaluated domains of HRQoL. The bachelor thesis may be of benefit to the cardio-centres and the cardiology departments. The results of the research may contribute to better understanding of the patients by the staff, to improve the hospital care and to widen the patients´ knowledge of this fact. A colloquium for the nursing staff aimed at the quality of life of patients suffering from a cardiovascular disease could be organized. The thesis may also be used to stimulate further research in comparing the quality of life dependent on different types of replacements or on the age of the patients.
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Injuries in Seniors and the Possibilities of their Prevention
Eklová, Pavla ; Čelko, Alexander (advisor)
The topic of my thesis "Accidents seniors and Prevention" I chose, because I know from experience that this is a very important and current issues. Injuries in this age group are common and may have for the elderly, as well as for its surroundings and caregivers, severe consequences in the form of sudden loss of significant limitations to its sovereignty and quality of life. Is not without significance or economic aspect. many such injuries could yet could be easily avoided if they had been given sufficient attention to the possibilities of their prevention. To fix the "awareness" of these options would help my work. In this work I tried to put the available resources together the most comprehensive view of this issue, including some concrete examples of the mentioned seemed appropriate. Statistical data for this work comes from the official outputs of the Czech Statistical Office, Department of Health Information and Statistics of the Czech Republic and the World Health Organization
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Analysis of clients of "House of three wishes" and their family background
Škodová, Klára ; Pazlarová, Hana (advisor) ; Turnovská, Elena (referee)
Diploma thesis "Analysis of Dům tří přání clients and their family background" presents the current system of care for children at risk in the historical development of children`s rights protection, social-legal protection of children; actual concept of particular departments, state administration, and non-government sector. The social-legal protection of children in the Czech Republic is segmental and is not enough to guarantee children`s rights to live in their biological families in case of support shortage. The forthcoming transformation and unification of the system of care for children is a great appeal for improving the cooperative work of all concerned in this field. One of the important element of the system, acting as a part of prevention of putting children into the institutions with constitutional education, is the civil association "Dům tří přání" which is authorized in providing the social-legal protection of children, and devices for children requiring immediate help. With the help of analysis of family background of children who are the clients of "Dům tří přání", and processing of selected statistical data, the given diploma thesis specifies some functional methods of working with children at risk and their families, directed to the safe family background and child`s development in the family.
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Control Problems in Epidemiology
Čížek, Pavel ; Pražák, Dalibor (referee) ; Milota, Jaroslav (advisor)
Na/.ev prace; Ki/cnf \) eh modeled] Aulor: Pavel Ci/ek Kaledra; Kaledra matemaliekc analy/.y Vcdouef bakala'rskc prace: Doc. KNDr. Jarosla\. CSc. c-inait vedouci'ho: niilota(« karlin.mff.cuni.c/ Ahsirakl: V predlo/cne praci studujeme model maso\. inlekcm mikropara/iiicke epidcinie. Co oduv.eni" modeiu, klcre \ycha/( / hiologickyeh po/nulku o sludovaiicni lypu epideiuii. u\a\liine |eho /a'kladm nialeniaiicke \htslmMi. /.axx'dcni'in ock(i\';ii:i' niotlei iransloriiiujcrnc. I);ile ^o /ah\\anie \laslnosUni feseni piivodm'ho i iransiorinox anelio niodelu a siahililou siaciona'nueli Inidii. PoroMuixanfni vysiedkii pro model puvodm a model iran>Jormovan\, /da je ocko\ain' /.a\edeno spra\-nc. lA.idinie i jiiie mo/noMi jcho /a\'edem. N;is!cdnc se /.ahvvanie cenou Icehy a ockovant'. Illedamc linancne n e j \ i re^cnf ma/k\k \'clikou cast populace oekovat. Tiile; Isi/em \h modeled! Auihor: Pa\el C ' f / e k Departnicnl: Kaledra iimlematickr aiialv/y Sii|)er\: Doe. RNDr. Jaio^lax Miloia. C'Se. Super\s e-mail adress: nii]o{a('1''karliu.n)tT.cuni.c/ Ahsii'acl: In the present work \\ studx a model of a ma^-action mieniparasiue epidoniic. After the deduction of llie motlel. \\lilcli issues from biologic in for uiafioii ahiui! ihe studied l\pe of epidemic. \\ mention basic maihematic.il chaiactcrislies. \\"e transform die...
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Mathematical Models for Biology
Hruška, Zdeněk ; Pražák, Dalibor (referee) ; Kaplický, Petr (advisor)
Na/.ev pracc: Matematieke modcly v biologii Autor: Zdenek Hruska Katedra: Vedoucf bakalafskc pracc: Mgr. Pctr Kaplicky, Ph.D. e-mail vcdouciho: kaplickyfV/Jkarlin.mff.cuni.cz Abstrakt: Modelovani epidcmii bylo prvnfm / ninoha pfipadu. kdy matematika vstoupila na pole biologic a mediciny. Infckcni cpidemicke ncmoci provazcjf lidstvo od samych pocatku historic a dodnes jsou vclmi zava/nym tcmatem nejen lekafskc vcdy. Ncktere z techto modelu be za velmi specifickych pfedpokladu popsat pomoci soustav obecne nclinearnich diferencialnich rovnic a vysetfovat jcjich kvalitativni vlastnosti jako jc jcjich existence, jednoznacnost a stabilita jcjich feseni. Nektcrc z techto ryzc matematickych vlastnosli systcmu jsou pak velmi blizke vlastnostcm populace realnclio svcta - podstatou modelu je prolo co nejvicc se pfiblizit parametrum skutccnosti, nebol" l/e z nej nejen pro lekafskou praxi vyefst cenne infonnacc. Pfi modelovani cpidcmickych proeesu tedy neni dulezite jen porozumet podslate chorob, ale take pomoci urcit odpovi'dajiei opatfcnf vcctnc oekovaci strategic. Klfcova slova: diferencialni rovnicc, soustavy, biologic Title: Mathematical models in biology Author: /denek Hruska Department: Supervisor: Mgr. Petr Kaplicky, Ph.D. Supervisor's e-mail: kaplickyCoJkarlin.mff.cuni.cz Abstract: The modelling of epidemics...
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Morphology and development of the midgut pathogens in bark beetle
TONKA, Tomáš
The bark beetle, Ips typographus is economically important pest of spruce standings across Europe. The knowledge of biology and ecology of bark beetles is important to protect spruce forests against beetles outbreaks. The research of pathogens of bark beetles is the main goal to use biological control of bark beetles and replace chemical or mechanical methods using today. During the bark beetle outbreak in Sumava mountains three main pathogens showed up very promising. Microsporidium Chytridiopsis typographi, the virus Ips typographus Entomopoxvirus and negregarine Menzbieria chalcographi were the most occured pathogens attacking beetles in Sumava outbreak area. Transmission of microspo ridium and virus have been introduced and propagated in living bark beetles in labo ratory. The reaserach of biology, transmission, morphogenesis and ultrastructure of these pathogens begun in living beetles in laboratory conditions. Results which were obtained can be divided to virological and microsporidian parts. In both cases the infection and routine passage have been successful in laboratory condition and now the infections of microsporidium Ch. typographi nad ITEV are routinely propagated to purchase infected material. Unlike the original description of ITEV in laboratory infected beetles the synthesis and origin of microspindles was described. In TEM the first steps of newly formed virions occluded into the spheroid were observed, including microspindles occlusion. ITEV develops in midgut epithelium of host. The successful infection of Ch. typographi has been managed in laboratory. Obtai ned results completed and revised findings which were published in first descriptions. Purchased results offer a possibility to compare old a new findings concernig this microsporidium. Budding as a unique process of multiplication has been described in microsporidia. This process is uncommon in microsporidia and has not never been observed. It acts as a tool to multiple vegetative stages in the life cycle. The ultrastructures and complete life cycle was described in Ch. typographi and the former description was revised.
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Detection and comparison of stability of compost with respirometer for different types of piles.
ONDRÁČEK, Vojtěch
The aim of this work was to verify the suitability of the device Ramko 2 for measuring the biological stability during the composting in terms of the Department of Agricultural Engineering. For this purpose were based four piles four piles with a similar composition and on which were measured temperature and DRI during all stages of composting. From the recorded data was created graphs both processes individual piles and compared with each other. From results assess the suitability for the authentication of biological stability.
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