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Synthesis of bisquaternary asymmetrical reactivators of acetylcholinesterase
Komlóová, Markéta ; Doležal, Martin (advisor) ; Kuča, Kamil (referee)
Markéta Komlóová: Synthesis of bisquarternary asymmetrical reactivators of acetylcholinesterase Nine potential bisquaternary reactivators of AChE have been prepared and their reactivation activity against paraoxon or tabun-inhibited enzyme has been tested in vitro. Three reactivators of AChE proved to be suitable for further testing against paraoxon. One of these compounds also demonstrated satisfactory efficiency when reacting against tabun. The reactivation abilities of prepared compounds depend on structural factors such as the presence of oxime group, its location, the presence of quaternary nitrogen and other functional groups. Also four monoquaternary inhibitors have been prepared and their inhibitive activity tested in vitro.
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Synthesis of 5-nitrosalicylanilide derivatives with potential antibacterial activity (Syntéza 5-nitrosalicylanilidových derivátů s potenciální antibakteriální aktivitou)
Kourtidou, Maria ; Vinšová, Jarmila (advisor) ; Komlóová, Markéta (referee)
Kourtidou Maria Synthesis of 5-nitrosalicylanilide derivatives with potential antibacterial activity Diploma thesis Charles University in Prague, Faculty of Pharmacy in Hradec Kralove Pharmacy Background: The aim of this diploma thesis was the synthesis of 5- nitrosalicylanilide derivatives as a potential anti-tuberculosis agent. Methods: The reactions were monitored, and the purity of products was verified by thin layer chromatography in which the plates were coated with silica gel 60 F254 and seen by using UV irradiation. Column chromatography was done using silica gel 60. The melting points of produced compounds were shown on a Melting Point apparatus, IR spectra were recorded using the technique of ART and the NMR spectra were measured in CDCl3 or DMSO-d6 Results: The starting compounds were generally reacted with success under the presence of chlorobenzene, trimethylamine and phosphorus trichloride and the microwave reactor. Conclusion: Unfortunately the final products of these experiments had impurities of phenolate salts.
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Synthesis of 5-nitrosalicylanilide derivatives with potential antibacterial activity (Syntéza 5-nitrosalicylanilidových derivátů s potenciální antibakteriální aktivitou)
Kourtidou, Maria ; Vinšová, Jarmila (advisor) ; Komlóová, Markéta (referee)
Kourtidou Maria Synthesis of 5-nitrosalicylanilide derivatives with potential antibacterial activity Diploma thesis Charles University in Prague, Faculty of Pharmacy in Hradec Kralove Pharmacy Background: The aim of this diploma thesis was the synthesis of 5- nitrosalicylanilide derivatives as a potential anti-tuberculosis agent. Methods: The reactions were monitored, and the purity of products was verified by thin layer chromatography in which the plates were coated with silica gel 60 F254 and seen by using UV irradiation. Column chromatography was done using silica gel 60. The melting points of produced compounds were shown on a Melting Point apparatus, IR spectra were recorded using the technique of ART and the NMR spectra were measured in CDCl3 or DMSO-d6 Results: The starting compounds were generally reacted with success under the presence of chlorobenzene, trimethylamine and phosphorus trichloride and the microwave reactor. Conclusion: Unfortunately the final products of these experiments had impurities of phenolate salts.
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Synthesis of salicylanilide esters with antibacterial activity
Alabed, Anwar ; Vinšová, Jarmila (advisor) ; Komlóová, Markéta (referee)
Alabed, Anwar. Synthesis of salicylanilide esters with antibacterial activity Hradec Králové, Faculty of Pharmacy, Charles University, 2013 This diploma thesis is concerned with synthesis of salicylanilides and their esters. Namely N-[4-Brom-3-(trifluormethyl)phenyl]-5chloro-2-hydroxybenzamide and N-[3,5 Bis(trifluormethyl)phenyl]-5-chloro-2-hydroxybenzamide were produced and then we tried to synthesize thein esters as isonicotinates and pyrazincarboxylates to enlarge the series of salicylanid esters for structure - antibacterial aktivity studies. This thesis summarizes the problems with tuberculosis, its therapy, development and modern therapy in preclinic and clinic phase, which has potencial to treat TBC. Most of this thesis is concerned with salicylanilides, their potential and problems.
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Relationship between Structure and Biological Activity of new Modulators of Acetylcholinesterase
Komlóová, Markéta ; Doležal, Martin (advisor) ; Kuneš, Jiří (referee) ; Jampílek, Josef (referee)
Charles University in Prague, Faculty of Pharmacy in Hradec Králové Department: Dpt. of Pharmaceutical Chemistry and Drug Control Student: Mgr. Markéta Komlóová Supervisor: prof. PharmDr. Martin Doležal, Ph.D. Title of Doctoral Thesis: Relationship between structure and biological activity of new modulators of acetylcholinesterase This work focuses on the preparation of peripherally acting AChE inhibitors as a potential treatment of myasthenia gravis. These compounds could also be used as a pre- treatment of poisoning by organophosphorus AChE inhibitors. They can occupy the active site of an enzyme making it inaccessible for irreversible inhibitors. Compounds used in this indication should fulfill these requirements: inhibit efficiently AChE (standards currently used in the treatment were chosen for the comparison of the inhibitory efficacy), have selective effect on AChE and not to cross the blood-brain barrier in order to lower the possible side effects. Six series of bisquaternary compounds were prepared. Their inhibitory ability was determined in vitro against human erythrocyte or recombinant AChE and human plasmatic BChE. According to inhibitory ability values acquired, a structure - activity relationships were investigated in every series. A few compounds with significant affinity towards...
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Synthesis of bisquaternary asymmetrical reactivators of acetylcholinesterase
Komlóová, Markéta ; Doležal, Martin (advisor) ; Kuča, Kamil (referee)
Markéta Komlóová: Synthesis of bisquarternary asymmetrical reactivators of acetylcholinesterase Nine potential bisquaternary reactivators of AChE have been prepared and their reactivation activity against paraoxon or tabun-inhibited enzyme has been tested in vitro. Three reactivators of AChE proved to be suitable for further testing against paraoxon. One of these compounds also demonstrated satisfactory efficiency when reacting against tabun. The reactivation abilities of prepared compounds depend on structural factors such as the presence of oxime group, its location, the presence of quaternary nitrogen and other functional groups. Also four monoquaternary inhibitors have been prepared and their inhibitive activity tested in vitro.
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