National Repository of Grey Literature 247 records found  1 - 10nextend  jump to record: Search took 0.01 seconds. 
Pyrazine derivatives as potential drugs III
Hošťálková, Anna ; Doležal, Martin (advisor) ; Kopecký, Kamil (referee)
Deriváty pyrazinu jako potanciální léčiva III. Tuberkulóza je problém v celosvětovém měřítku. Rostoucí počet nakažených lidí, vznik lékově rezistentních kmenů Mycobacterium tuberculosis a ko-infekce HIV vedly k naléhavé potřebě nových antituberkulotik. Tato diplomová práce referuje o současných léčivech používaných při léčbě tuberkulózy a některých nových potenciálních antituberkuloticích. Také bylo v rámci diplomové práce syntetizováno deset nových látek, derivátů anilidů kyseliny pyrazin-2-karboxylové, které byly charakterizovány jejich fyzikálními vlastnostmi a poté byla zkoušena jejich antimykobakteriální a antifungální aktivita in vitro. Abstract Pyrazine derivatives as potential drugs III. Tuberculosis is a health problem worldwide. The increasing number of infected people, emergence of drug resistant strains Mycobacterium tuberculosis and HIV co-infection have resulted in the urgent need for new antituberculosis drugs. This degree work reviews drugs used in current treatment for tuberculosis and some of new potential anti-tuberculosis drug candidates. Within the task of this work were also synthesized ten new compounds, derivatives of anilides of pyrazin-2-carboxylic acid, which were characterized by physical properties and then was assayed their antimycobacterial and antifungal activity in...
Pyrazine Derivates as Potential Antituberculotic Drugs
Kačírek, Michal ; Doležal, Martin (advisor) ; Kopecký, Kamil (referee)
Title of rigorous thesis: Pyrazine derivates as potential antituberculotic drugs Author: Mgr. Michal Kačírek In this rigorous thesis the recherche was realized which was focused on recent incidence of tuberculosis in the world, the possibility o f present therapy and the new trends in therapy as well. This thesis dealt with synthesis of undocumented compounds in literature. The starting compound was 5-chloro-6-methylpyrazine-2,3- dicabronitrile. The compounds were developed by aminodehalogenational reaction, linked to alkyl descriptor across amino group, whereas side chains were anal ogously extended. It can be said that the product was developed by reaction of 5 -chloro-6- methylpyrazine-2,3-dicabronitrile with corresponding primary aliphatic amine. Final compounds were characterized by thaw point, TLC, elementary analysis, 1 H a 13 C NMR and IR. All compounds were liable in vitro testing on their biological activity - antimycobacterial, antifungal and antibacterial. In the group of antituberculosis test ing the activity grew up from the least to the most lipophility compound.
Intracellular trafficking of an anti - Amyloid Protein Precursor antibody.
Zitko, Jan ; Doležal, Martin (advisor) ; Trejtnar, František (referee)
Intracellular trafficking of an anti-Amyloid Protein Precursor antibody Alzheimer's disease is characterized by over-accumulation of beta-amyloid peptide (Aβ) in the brain. Aβ is produced by proteolytic cleavage of beta-amyloid precursor protein (APP) by β- and γ-secretases. Novel monoclonal antibody, 2B12, has been shown to bind to β-secretase cleavage site of APP, reducing the production of APP, presumably by preventing the cleavage by steric hindrance. 2B12 is hypothesized to bind to APP molecules exposed on the cell surface and to be internalized in the form of complex with APP via natural endocytic pathway. This hypothesis was confirmed by San Pei Ho's (2007), who followed the internalization of 2B12 in living astrocytoma MOG-G-UVW, cells in time-course experiment. This project is focused on intracellular trafficking of 2B12 and its localization within specific cellular compartments. Experiments were performed with fixed astrocytoma MOG- G-UVW cells (constitutively expressing APP). Originally planned experiments with live cells could not be performed due to decreased stability of 2B12 (causes remain unknown). 2B12 was tested for colocalization with polyclonal affinity purified antibodies labelling subcellular markers (proteins) associated with compartments known to participate in APP...
The Synthesis of Unsymmetrical Azaphthalocyanines via Transetherification
Franzová, Šárka ; Zimčík, Petr (advisor) ; Doležal, Martin (referee)
The synthesis of unsymmetrical azaphthalocyanines via transetherification Mgr. Šárka Franzová Department of Pharmaceutical Chemistry and Drug Control, Faculty of Pharmacy in Hradec Kralove, Charles University in Prague The introduction of a functional group on the periphery of substituted aryloxy azaphthalocyanines (AzaPc) seems to be very promising because it allows binding AzaPc to biomolecules. Common synthetic methods giving symmetrical molecules cannot be used for unsymmetrical aryloxy AzaPc derivatives, because alkoxides, which are used as initiators of cyclization reactions, cause transetherification due to strongly electron-deficient carbons 5 and 6 of pyrazine-2,3-dicarbonitrile, the precursors for AzaPc. This work describes two reaction methods leading to the synthesis of planar substituted aryloxy AzaPc. The first method was based on a template effect of the central metal. However, low yields resulted to change of the concept for introduction a functional group on the periphery AzaPc. The cyclization in butanol with magnesium butoxide, which was originally precluded due to adverse transetherification reaction, was successfully used for unsymmetric AzaPc preparation bearing one functional group in the molecule. This process, called controlled transetherification, seems to be a promising method for...
Sulfonated azaphthalocyanines - synthesis and evaluation of their photodynamic activity
Jančárová, Alena ; Zimčík, Petr (advisor) ; Doležal, Martin (referee)
Charles University Faculty of Pharmacy in Hradec Králové Department of Pharmaceutical Chemistry and Pharmaceutical Analysis Author: Alena Jančárová Supervisor: doc. PharmDr. Petr Zimčík, Ph.D. Co-supervisor: RNDr. Miloslav Macháček, Ph.D. Title of diploma thesis: Sulfonated azaphthalocyanines - synthesis and evaluation of their photodynamic activity Photodynamic therapy is one of the methods used for destruction of undesirable cells. It combines three essentially nontoxic components: light, oxygen and a photosensitizer. Azaphthalocyanines (AzaPcs) are promising compounds with photosensitizing properties. However, their major disadvantage is their low water solubility and significant aggregation that decreases their photodynamic activity. The aim of this work was to synthesize an anionic derivative of AzaPc substituted with sulfonic groups on periphery characterized by good solubility in water and to evaluate its photodynamic properties. The first step in the synthesis was condensation of diaminomaleonitrile with benzil giving 5,6-diphenylpyrazine-2,3-dicarbonitrile. Subsequently, the cyclotetramerisation with zinc acetate in 2-dimethylaminoethanol as a solvent was performed. The final product was obtained by sulfonation with chlorosulfonic acid followed by hydrolysis with sodium hydrogen carbonate....

National Repository of Grey Literature : 247 records found   1 - 10nextend  jump to record:
See also: similar author names
3 Doležal, Marek
6 Doležal, Michal
3 Doležal, Milan
4 Doležal, Miroslav
Interested in being notified about new results for this query?
Subscribe to the RSS feed.