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Chemistry of polynitro heterocyclic compounds
Kubátková, Nela ; Bednařík, Karel (referee) ; Friedl, Zdeněk (advisor)
The review of polynitro heterocyclic compounds was written. These are substances with ability to detonate, which is caused mainly by presence of nitrogroups, which are bonded to carbon atoms in their cycles. The thesis deals with common polynitro five-membered heterocycles with one nitro atom, up to six-membered heterocycles with three nitrogen atoms. There are processed basic information of these compounds, as well as their physical-chemical properties and properties of detonation, the possibility of their preparation, which are displayed in the form of chemical reactions.
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The effect of pyrazine derivatives on secondary metabolites content in plant cultures in vitro - III.
Blahnová, Kristýna ; Tůmová, Lenka (advisor) ; Karlíčková, Jana (referee)
One of the possibilities how to increase the production of secondary metabolites (SM) in plant in vitro cultures is the method of elicitation. The aim of this work was to determine the effect of an abiotic elicitor from the class of pyrazine derivatives 1-benzyl-3-(pyrazin-2-yl)urea on the production of flavonolignans of silymarin complex and flavonoid taxifolin in the plant culture Silybum marianum (L.) Gaertn. Pyrazine derivatives are investigated for their herbicidal properties, so elicitation proceeds by the mechanism of stress inducing effect. Tissue cultures were grown on Murashige and Skoog growth medium with the addition of the growth regulator α-naphthylacetic acid. Elicitation was performed on both callus and suspension cultures. The elicitor was used in three different concentrations: c1 = 100.0 mg/100 ml; c2 = 10.0 mg/100 ml; c3 = 1.00 mg/100 ml. Particular samples were taken after 6, 24, 48, 72 and 168 hours of elicitor effect, control samples after 6, 48 and 168 hours. After drying, the callus and suspension tissues were extracted with methanol and the content of the monitored secondary metabolites was determined by HPLC. It was also tested if SM are released into the growth medium. Flavonolignans silybinin A and silybinin B were not detected in any of the analyzed samples. The...
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The effect of pyrazine derivatives on secondary metabolites content in plant cultures in vitro - III.
Blahnová, Kristýna ; Tůmová, Lenka (advisor) ; Karlíčková, Jana (referee)
One of the possibilities how to increase the production of secondary metabolites (SM) in plant in vitro cultures is the method of elicitation. The aim of this work was to determine the effect of an abiotic elicitor from the class of pyrazine derivatives 1-benzyl-3-(pyrazin-2-yl)urea on the production of flavonolignans of silymarin complex and flavonoid taxifolin in the plant culture Silybum marianum (L.) Gaertn. Pyrazine derivatives are investigated for their herbicidal properties, so elicitation proceeds by the mechanism of stress inducing effect. Tissue cultures were grown on Murashige and Skoog growth medium with the addition of the growth regulator α-naphthylacetic acid. Elicitation was performed on both callus and suspension cultures. The elicitor was used in three different concentrations: c1 = 100.0 mg/100 ml; c2 = 10.0 mg/100 ml; c3 = 1.00 mg/100 ml. Particular samples were taken after 6, 24, 48, 72 and 168 hours of elicitor effect, control samples after 6, 48 and 168 hours. After drying, the callus and suspension tissues were extracted with methanol and the content of the monitored secondary metabolites was determined by HPLC. It was also tested if SM are released into the growth medium. Flavonolignans silybinin A and silybinin B were not detected in any of the analyzed samples. The...
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The effect of pyrazine derivatives on the secondary metabolites production in in vitro cultures of medicinal plants I.
Dvořáková, Jana ; Tůmová, Lenka (advisor) ; Kašparová, Marie (referee)
The aim of this work was to investigate the effect of pyrazine derivative, 1-octyl-3-(pyrazin-2- yl)urea, as an abiotic elicitor on the production of flavonoid rutin in in vitro cultures of Fagopyrum esculentum Moench., Cultivar Bamby. Suspension and callus cultures were cultivated on Murashige and Skoog nutrient medium (MS) with the addition of 2,4-dichlorophenoxyacetic acid (2,4-D) as growth regulator at a concentration of 1 mg/l. The elicitor solution was added to the cultures at three concentrations: c1 (100,0 mg/100 ml), c2 (10,0 mg/100 ml) and c3 (1,0 mg/100 ml). The elicitor was monitored at six time intervals: 6, 12, 24, 48, 72 and 168 hours. To control samples 1 ml of ethanol 96% was added instead of elicitor solution and samples were collected after 24 and 168 hours. Samples were taken at given time intervals and dried. Subsequently, the rutin content was monitored by HPLC. The rutin release into the nutrient medium was also tested. During the experiment on the callus cultures no statistically significant increase in rutin production after elicitor treatment was observed. But elicitor increased rutin production in suspension cultures after treatment in all tested concentrations. The calluses always released rutin into the nutrient medium. The rutin content in the media ranged from 53,4 to...
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Derivatives of pyrazine as potencial antitubercular drugs
Dobrovolný, Lukáš ; Doležal, Martin (advisor) ; Hartl, Jiří (referee)
Charles University in Prague, Faculty of Pharmacy in Hradec Králové Department of Pharmaceutical chemistry and drug control Candidate Mgr. Lukáš Dobrovolný Consultant Doc. PharmDr. Martin Doležal, Ph.D. Title of Thesis Derivates of pyrazine as antitubercular drugs Pyrazinamide (PZA) as a traditional antitubercular drug and quite simple molecul offers many possibilities to change its structure. Thaťs the way how to gain more entities with greater antitubercular potency. The series of 14 not yet described compounds have been synthetised. All of them were derived from 3-chloropyrazine- 2,5-dicarbonitrile by nuclephilic substitution with non-aromatic amines (i.e. aliphatic, cycloaliphatic, eventually heterocyclic) in position 3. The prepared substances were put to in vitro antimycobacterial, antibacterial and antifungal testing. The highest aliphatic analogues manifested supreme activity against M. tuberculosis H37Rv, whereas 3-heptylaminepyrazine-2,5-dicarbonitrile achieved the best outcome comparable with PZA recalculated to MIC 12,5 µg/ml. Moreover, few substances (especially 3-hexylaminepyrazine-2,5- dicarbonitrile) manifested activity against M. kansasii and M. avium, which are meant to be unsusceptible to PZA. No antibacterial and just irrelevant antimycotic activity was detected. The molecules...
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Chemistry of polynitro heterocyclic compounds
Kubátková, Nela ; Bednařík, Karel (referee) ; Friedl, Zdeněk (advisor)
The review of polynitro heterocyclic compounds was written. These are substances with ability to detonate, which is caused mainly by presence of nitrogroups, which are bonded to carbon atoms in their cycles. The thesis deals with common polynitro five-membered heterocycles with one nitro atom, up to six-membered heterocycles with three nitrogen atoms. There are processed basic information of these compounds, as well as their physical-chemical properties and properties of detonation, the possibility of their preparation, which are displayed in the form of chemical reactions.
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